标签归档：acetate

H-D-Phe-Pip-Arg-pNA acetate(Synonyms: S-2238 acetate)

发表于由
回复

H-D-Phe-Pip-Arg-pNA acetate;(Synonyms: S-2238 acetate) 纯度: 98.14%

H-D-Phe-Pip-Arg-pNA (S-2238) acetate 是一种显色底物，在凝血酶的天然底物纤维蛋白原 α 链的 N 端部分之后形成。H-D-Phe-Pip-Arg-pNA acetate 对凝血酶有特异性，用于测定抗凝血酶肝素辅因子 (AT-III)。使用 H-D-Phe-Pip-Arg-pNA acetate 进行的 AT-III 分析灵敏、准确、易于执行。

H-D-Phe-Pip-Arg-pNA acetateamp;;(Synonyms: S-2238 acetate)

H-D-Phe-Pip-Arg-pNA acetate Chemical Structure

CAS No. : 115388-96-0

规格 价格 是否有货 数量
5 mg ￥4000 In-stock
10 mg ￥6800 In-stock
25 mg ￥13500 In-stock
50 mg ￥22000 In-stock
100 mg ￥34000 In-stock
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

H-D-Phe-Pip-Arg-pNA acetate 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus

生物活性

H-D-Phe-Pip-Arg-pNA (S-2238) acetate, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA acetate is specific for thrombin and is used to measure antithrombin-heparin cofactor (AT-III). The AT-III assay using H-D-Phe-Pip-Arg-pNA acetate is sensitive, accurate, and easy to perform[1][2].

分子量

612.68

Formula

C29H40N8O7
CAS 号

115388-96-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (163.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6322 mL 8.1609 mL 16.3217 mL
5 mM 0.3264 mL 1.6322 mL 3.2643 mL
10 mM 0.1632 mL 0.8161 mL 1.6322 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (4.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.08 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.08 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Goodnight SH Jr, et al. Measurement of antithrombin III in normal and pathologic states using chromogenic substrate S-2238. Comparison with immunoelectrophoretic and factor Xa inhibition assays. Am J Clin Pathol. 1980;73(5):639-647.

    [2]. Voorthuizen H, Kluft C. Improved assay conditions for automated antithrombin III determinations with the chromogenic substrate S-2238. Thromb Haemost. 1984;52(3):350-353.

Euphol acetate

发表于由
回复

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Euphol acetate 

Euphol acetate 是一种三萜烯类化合物，可以从 Euphorbia broteri 中提取得到。Euphol acetate 是肝转运蛋白 OATP1B1/3 的抑制剂。

Euphol acetate

Euphol acetate Chemical Structure

CAS No. : 13879-04-4

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3)[1][2].

IC50 & Target

OATP1B1/3[2]
体外研究
(In Vitro)

Euphol acetate (10 μM) suppresses the uptake of the OATP1B substrate sodium fluorescein in OATP1B1 (29.2%)- or 1B3 (40.2%)-transfected CHO cells[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

468.75

Formula

C32H52O2
CAS 号

13879-04-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. DePascual Teresa, et al. Triterpenes from Euphorbia broteri. Phytochemistry. 1987. 26(6): 1767-1776.

    [2]. Tom De Bruyn, et al. Structure-based identification of OATP1B1/3 inhibitors. Mol Pharmacol. 2013 Jun;83(6):1257-67.

Rusalatide acetate(Synonyms: TP508 amide acetate)

发表于由
回复

Rusalatide acetate;(Synonyms: TP508 amide acetate) 纯度: 98.26%

Rusalatide acetate (TP508 amide acetate) 是一种再生肽，能够激活干细胞再生修复以及保护隐窝完整性，达到减缓辐照引起的胃肠道损伤。

Rusalatide acetateamp;;(Synonyms: TP508 amide acetate)

Rusalatide acetate Chemical Structure

CAS No. : 875455-82-6

规格 价格 是否有货 数量
1 mg ￥2100 In-stock
5 mg ￥4800 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Rusalatide acetate 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Rusalatide acetate (TP508 amide acetate), a regenerative peptide, mitigates radiation-induced gastrointestinal damage by activating stem cells and preserving crypt integrity[1].

体外研究
(In Vitro)

Rusalatide (TP508) is a 23 amino acid peptide representing amino acids 508-530 of human prothrombin that was identified as the high-affinity binding domain of thrombin responsible for interaction with a subset of thrombin receptors on the surface of fibroblasts thought to initiate tissue repair[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

2371.50

Formula

C99H151N29O37S
CAS 号

875455-82-6
Sequence Shortening

AGYKPDEGKRGDACEGDSGGPFV-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture and light

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture and light)
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Kantara C, et al. Novel regenerative peptide TP508 mitigates radiation-induced gastrointestinal damage by activating stem cells and preserving crypt integrity. Lab Invest. 2015 Nov;95(11):1222-33.

Tetracosactide acetate(Synonyms: Tetracosactrin acetate)

发表于由
回复

Tetracosactide acetate;(Synonyms: Tetracosactrin acetate) 纯度: 99.49%

Tetracosactide acetate 是一种合成肽，可刺激肾上腺释放皮质类固醇 (如皮质醇)。Tetracosactide acetate 目前用于溃疡性结肠炎和克罗恩病、青少年/成人类风湿性关节炎和骨关节病的研究。

Tetracosactide acetateamp;;(Synonyms: Tetracosactrin acetate)

Tetracosactide acetate Chemical Structure

CAS No. : 60189-34-6

规格 价格 是否有货 数量
5 mg ￥2500 In-stock
10 mg ￥3900 In-stock
25 mg ￥7800 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Tetracosactide acetate 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Tetracosactide acetate is a synthetic peptide stimulating the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide acetate is currently used for the research of ulcerative colitis and Crohn’s disease, juvenile/adult rheumatoid arthritis and osteoarthrosis[1].

Formula

C2H4O2
CAS 号

60189-34-6
Sequence Shortening

SYSMEHFRWGKPVGKKRRPVKVYP
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
参考文献

  • [1]. Francesco Iuliano, et al. Adding Slow Release Tetracosactide Acetate to Eltrombopag Improves Haematological Response in ITP Patients with Platelet-Count Fluctuation.

IYPTNGYTR acetate

发表于由

IYPTNGYTR acetate; 纯度: 99.41%

IYPTNGYTR acetate，一种脱酰胺敏感的特征肽，是曲妥珠单抗 (Trastuzumab) 的脱酰胺产物。 IYPTNGYTR acetate 可用于监测体内曲妥珠单抗的代谢。

IYPTNGYTR acetateamp;;

IYPTNGYTR acetate Chemical Structure

规格 价格 是否有货 数量
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

IYPTNGYTR acetate 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Drug Metabolite Library
  • Peptide Library

生物活性

IYPTNGYTR acetate, a deamidation-sensitive signature peptide, is a deamidation product of Trastuzumab. IYPTNGYTR acetate can be used to monitor in vivo Trastuzumab metabolism[1].

体外研究
(In Vitro)

IYPTNGYTR is deamidated at pH 7.5 and above, with a higher deamidation rate when the pH increases[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1144.23

Formula

C51H77N13O17
Sequence Shortening

IYPTNGYTR
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

H2O : 125 mg/mL (109.24 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8740 mL 4.3698 mL 8.7395 mL
5 mM 0.1748 mL 0.8740 mL 1.7479 mL
10 mM 0.0874 mL 0.4370 mL 0.8740 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Bults P, et, al. LC-MS/MS-Based Monitoring of In Vivo Protein Biotransformation: Quantitative Determination of Trastuzumab and Its Deamidation Products in Human Plasma. Anal Chem. 2016 Feb 2;88(3):1871-7.

Pramlintide acetate(Synonyms: 普兰林肽醋酸盐)

发表于由

Pramlintide acetate;(Synonyms: 普兰林肽醋酸盐) 纯度: 98.66%

Pramlintide acetate 是一种人胰淀粉样多肽类似物。Pramlintide acetate 是一种抗糖尿病剂，也可用于肠癌的研究。

Pramlintide acetateamp;;(Synonyms: 普兰林肽醋酸盐)

Pramlintide acetate Chemical Structure

规格 价格 是否有货 数量
5 mg ￥1800 In-stock
10 mg ￥2800 In-stock
25 mg ￥6000 In-stock
50 mg ￥9600 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Pramlintide acetate 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Pramlintide acetate is a polypeptide analogue of human amylin. Pramlintide acetate, an antidiabetic agent, is antineoplastic in colorectal cancer[1].

体外研究
(In Vitro)

Pramlintide inhibits the growth of HCT-116 and HT-29 in a dose-dependent manner, with higher efficacy against the latter (IC50s of 48.67 and 9.10 μg/mL, respectively)[1].
The addition of 5, 10, and 20 μg/mL of Pramlintide to HCT-116 and HT-29 with 5-fluorouracil, Oxaliplatin, or Irinotecan induces the antiproliferative effect synergistically[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

4011.51

Formula

C173H273N51O55S2
Sequence

Lys-Cys-Asn-Thr-Ala-Thr-Cys-Ala-Thr-Gln-Arg-Leu-Ala-Asn-Phe-Leu-Val-His-Ser-Ser-NH2 (Disulfide bridge:Cys2-Cys7)
Sequence Shortening

KCNTATCATQRLANFLVHSSNNFGPILPPTNVGSNTY-NH2 (Disulfide bridge:Cys2-Cys7)
中文名称

普兰林肽醋酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

H2O : 50 mg/mL (12.46 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.2493 mL 1.2464 mL 2.4928 mL
5 mM 0.0499 mL 0.2493 mL 0.4986 mL
10 mM 0.0249 mL 0.1246 mL 0.2493 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Maha S Al-Keilani, et al. Pramlintide, an antidiabetic, is antineoplastic in colorectal cancer and synergizes with conventional chemotherapy. Clin Pharmacol. 2018 Mar 5;10:23-29.

α-Amyrin acetate

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

α-Amyrin acetate 

α-​Amyrin acetate，一种三萜类化合物，具有抗炎活性、抗痉挛特性和松弛作用。

α-Amyrin acetate

α-Amyrin acetate Chemical Structure

CAS No. : 863-76-3

规格 价格 是否有货
5 mg ￥5500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

α-Amyrin acetate, a natural triterpenoid, has anti-inflammatory activity, antispasmodic profile and the relaxant effect[1][2].

分子量

468.75

Formula

C32H52O2
CAS 号

863-76-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Okoye NN, et al. beta-Amyrin and alpha-amyrin acetate isolated from the stem bark of Alstonia boonei displayprofound anti-inflammatory activity. Pharm Biol. 2014 Nov;52(11):1478-86.

    [2]. Ali N. Brine shrimp cytotoxicity of crude methanol extract and antispasmodic activity of α-amyrin acetate from Tylophora hirsuta wall. BMC Complement Altern Med. 2013 Jun 17;13:135.

TAK-683 acetate

发表于由

TAK-683 acetate;

TAK-683 acetate 是一种有效的完全 KISS1R 激动剂 (IC50=170 pM)，具有改善的代谢稳定性。TAK-683 acetate 是一个九肽 metastin 的类似物，针对人与大鼠 EC50 值分别为 0.96 nM 和 1.6 nM。TAK-683 acetate 消耗下丘脑 GnRH，降低血浆 FSH、LH、睾酮水平，具有研究激素依赖性前列腺癌的潜力。

TAK-683 acetateamp;;

TAK-683 acetate Chemical Structure

规格 价格 是否有货 数量
1 mg ￥3500 In-stock
5 mg ￥8500 In-stock
10 mg ￥14500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

TAK-683 acetate 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][4].

体外研究
(In Vitro)

TAK-683 acetate exhibits an IC50 value (95% CI) from receptor binding assays is 150-180 pM and EC50 value (95% CI) from Ca+ mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

TAK-683 acetate (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced[3].
TAK-683 acetate (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer[3].
TAK-683 acetate (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SD rat with prostate cancer model[4]
Dosage: 2.1, 7, 14, 21 nmol/kg/day
Administration: Subcutaneous injection
Result: Exhibited a sustained testosterone suppression in rat.

分子量

1358.50

Formula

C66H87N17O15
Sequence Shortening

N-Acetyl-YWNTF{aza}L{Met-R}W-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light, stored under nitrogen

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:;

H2O : 5 mg/mL (3.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7361 mL 3.6805 mL 7.3611 mL
5 mM — — —
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Nishizawa N, et al. Design and Synthesis of an Investigational Nonapeptide KISS1 Receptor (KISS1R) Agonist, Ac-d-Tyr-Hydroxyproline (Hyp)-Asn-Thr-Phe-azaGly-Leu-Arg(Me)-Trp-NH2 (TAK-448), with Highly Potent Testosterone-Suppressive Activity and Excellent Water Solubility. J Med Chem. 2016 Oct 13;59(19):8804-8811. Epub 2016 Sep 21.

    [2]. Asami T, et al.Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.J Med Chem. 2013 Nov 14;56(21):8298-307.

    [3]. Hisanori MATSUI, et al. Functional Analyses of Kisspeptin in Controlling Gonadal Functions

JMV 449 acetate

发表于由

JMV 449 acetate; 纯度: 99.84%

JMV 449 acetate 是一种有效的神经降压素受体 (neurotensin receptor) 激动剂。JMV 449 acetate 显示抑制 125I-neurotensin 与新生小鼠脑结合的 IC50 为 0.15 nM，对收缩豚鼠回肠的 EC50 为 1.9 nM。JMV 449 acetate 对小鼠具有高效、持久的降温和缓解疼痛作用。

JMV 449 acetateamp;;

JMV 449 acetate Chemical Structure

规格 价格 是否有货 数量
5 mg ￥7000 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

JMV 449 acetate 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Neuronal Signaling Compound Library

生物活性

JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse[1][2].

体内研究
(In Vivo)

JMV 449 (120 pmol/mouse; i.c.v) shows analgesic effect[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Swiss albino mice[1]
Dosage: 120 pmol/mouse
Administration: I.c.v.
Result: Showed dose-response relation-ships for the analgesic effect.

分子量

807.03

Formula

C40H70N8O9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

H2O : 100 mg/mL (123.91 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2391 mL 6.1956 mL 12.3911 mL
5 mM 0.2478 mL 1.2391 mL 2.4782 mL
10 mM 0.1239 mL 0.6196 mL 1.2391 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Lugrin D, et al. Reduced peptide bond pseudopeptide analogues of neurotensin: binding and biological activities, and in vitro metabolic stability. Eur J Pharmacol. 1991;205(2):191-198.

    [2]. Dubuc I, et al. JMV 449: a pseudopeptide analogue of neurotensin-(8-13) with highly potent and long-lasting hypothermic and analgesic effects in the mouse. Eur J Pharmacol. 1992;219(2):327-329.

Plecanatide acetate(Synonyms: 普卡那肽醋酸盐；醋酸普卡那肽)

发表于由

Plecanatide acetate;(Synonyms: 普卡那肽醋酸盐；醋酸普卡那肽) 纯度: 99.26%

Plecanatide acetate 是尿鸟苷蛋白的类似物，是一种具有口服活性的鸟苷酸环化酶 C 受体 (guanylate cyclase-C (GC-C) receptor) 激动剂，在 T84 细胞中，EC50 值为 190 nM。Plecanatide acetate 可用于慢性特发性便秘的研究，在小鼠结肠炎模型中具有抗炎活性。

Plecanatide acetateamp;;(Synonyms: 普卡那肽醋酸盐；醋酸普卡那肽)

Plecanatide acetate Chemical Structure

CAS No. : 1075732-84-1

规格 价格 是否有货 数量
5 mg ￥4900 In-stock
10 mg ￥8500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Plecanatide acetate 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis[1][2][3].

IC50 Target

EC50: 190 nM (guanylate cyclase-C receptor, T84 cells)[1]
体外研究
(In Vitro)

Plecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cGMP synthesis in a dose-dependent manner with EC50 of 190 nM in T84 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Plecanatide (0.5 and 2.5 mg/kg, p.o.) ameliorates spontaneous and chemically induced colitis after treatment for 7 days in BALB/c mice, and 14 days in TCRα-/- mice[1].
Plecanatide (0.005-5 mg/kg, once daily for 7 days) also shows anti-inflammatory activity in dextran sulfate sodium (DSS) and trinitrobenzene sulfonic (TNBS)-induced colitis in BDF-1 mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (2-4 month old) are induced colitis by TNBS[1]
Dosage: 0, 0.5 and 2.5 mg/kg
Administration: P.o. for 7 days
Result: Effectively reduced colitis severity scores as compared to vehicle treatment.

Clinical Trial

分子量

1741.94

Formula

C67H108N18O28S4
CAS 号

1075732-84-1
Sequence

Asn-Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)
Sequence Shortening

NDECELCVNVACTGCL (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)
中文名称

普卡那肽醋酸盐；醋酸普卡那肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
参考文献

  • [1]. Shailubhai K, et al. Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis. World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):213-22.

    [2]. Rao SSC. Plecanatide: a new guanylate cyclase agonist for the treatment of chronic idiopathic constipation. Therap Adv Gastroenterol. 2018 Jun 8;11:1756284818777945.

    [3]. Shailubhai K, et, al. Plecanatide, an oral guanylate cyclase C agonist acting locally in the gastrointestinal tract, is safe. Dig Dis Sci. 2013 Sep;58(9):2580-6.