[Lys8, Lys9]-Neurotensin (8-13)(Synonyms: JMV438)

[Lys8, Lys9]-Neurotensin (8-13);(Synonyms: JMV438)

[Lys8, Lys9]-Neurotensin (8-13) (JMV438) 是神经降压素的类似物,通过激活 G 蛋白偶联受体 NTS1NTS2 来发挥作用,其对 hNTS1 和 hNTS2 受体的 Ki 值分别为 0.33 nM 和 0.95 nM,可用于缓解疼痛的研究。

[Lys8, Lys9]-Neurotensin (8-13)amp;;(Synonyms: JMV438)

[Lys8, Lys9]-Neurotensin (8-13) Chemical Structure

CAS No. : 139026-64-5

规格 是否有货
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250 mg ; 询价 ;
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生物活性

[Lys8, Lys9]-Neurotensin (8-13) (JMV438), a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2, with Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively[1].

分子量

761.00

Formula

C38H64N8O8

CAS 号

139026-64-5

Sequence Shortening

KKPYIL

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.

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]. Emilie Eiselt, et al. Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia. ACS Chem Neurosci. 2019 Nov 20;10(11):4535-4544.

[D-Trp11]-Neurotensin

[D-Trp11]-Neurotensin;

[D-Trp11]-Neurotensin 是 Neurotensin (NT) 的类似物,在灌注的大鼠心脏中是 NT 的选择性拮抗剂,但在豚鼠心房和大鼠胃条中起完全激动剂的作用。[D-Trp11]-Neurotensin 可抑制 NT 引起的低血压。

[D-Trp11]-Neurotensinamp;;

[D-Trp11]-Neurotensin Chemical Structure

CAS No. : 73634-68-1

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension[1][2].

IC50 Target

Neurotensin Receptor[1]

体外研究
(In Vitro)

[D-Trp11]-Neurotensin (0.13-1.1 μM) markedly inhibits NT-induced coronary vessel constriction in perfused rat hearts[1].
[D-Trp11]-Neurotensin (2-110 μM) exhibits NT-like activity in perfused rat hearts[1].

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

体内研究
(In Vivo)

[D-Trp11]-Neurotensin (50-500 nmol/kg; i.v.) has hypotensive activity in pentobarbital-anesthetized rats, with an ED25 of 122 nmol/kg[2].

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

分子量

1695.96

Formula

C80H122N22O19

CAS 号

73634-68-1

Sequence

{Pyr}-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-{D-Trp}-Ile-Leu

Sequence Shortening

{Pyr}-LYENKPRRP-{D-Trp}-IL

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.

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]. Quirion R, et, al. Selective blockade of neurotensin-induced coronary vessel constriction in perfused rat hearts by a neurotensin analogue. Eur J Pharmacol. 1980 Feb 8;61(3):309-12.

    [2]. Quirion R, et, al. Hypotensive effects of centrally and peripherally administered neurotensin and neurotensin derivatives in rats. Neuropeptides. 1981 Jou. 1(4): 253-9.

Neurotensin(Synonyms: 神经降压素)

Neurotensin;(Synonyms: 神经降压素) 纯度: 97.40%

Neurotensin 是一种肠十三肽,作为有效的细胞有丝分裂原,作用于各种结肠直肠癌和胰腺癌,对神经降压素受体 (neurotensin receptorNTR) 具有高亲和力。

Neurotensinamp;;(Synonyms: 神经降压素)

Neurotensin Chemical Structure

CAS No. : 39379-15-2

规格 价格 是否有货 数量
1 mg ¥500 In-stock
5 mg ¥1500 In-stock
10 mg ¥2100 In-stock
25 mg ¥4200 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

Neurotensin 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).

IC50 Target

Neurotensin receptors (NTR)[1]

体外研究
(In Vitro)

Neurotensin induces the expression of MIP-2, MCP-1, IL-1β and TNFα in murine microglial cells and stimulates IL-8 secretion in a non-transformed colon epithelial cell line stably transfected with the NTR. The high-affinity NTR, a member of the G-protein coupled receptor (GPCR) family, is present in a majority of human pancreatic and colorectal cancers, suggesting that Neurotensin (NT) may act in an endocrine fashion to affect tumor growth. Acting through the NTR1, Neurotensin is known to stimulate various signal transduction pathways, including intracellular calcium ([Ca2+]i), the mitogen-activated protein kinases (MAPKs), ERK and JNK, and various PKC isoforms. Treatment of HCT116 cells with Neurotensin (100 nM) significantly increases HCT116 cell migration (~3-fold) compared with vehicle treatment; pretreatment with Curcumin (10 μM) blocksthe stimulatory effect of NT on HCT116 cell migration. ctivation of MEK/ERK by NT and downstream induction of AP-1 transcription factors contributes to the proliferative effects of Neurotensin[1].

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

Clinical Trial

分子量

1672.92

Formula

C78H121N21O20

CAS 号

39379-15-2

Sequence

Pyr-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu

Sequence Shortening

Pyr-LYENKPRRPYIL

中文名称

神经降压素

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80deg;C 2 years
-20deg;C 1 year
In solvent -80deg;C 6 months
-20deg;C 1 month
溶解性数据
In Vitro:;

H2O : 33.33 mg/mL (19.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5978 mL 2.9888 mL 5.9776 mL
5 mM 0.1196 mL 0.5978 mL 1.1955 mL
10 mM 0.0598 mL 0.2989 mL 0.5978 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。-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]. Wang X, et al. Curcumin inhibits neurotensin-mediated interleukin-8 production and migration of HCT116 human colon cancer cells. Clin Cancer Res. 2006 Sep 15;12(18):5346-55.

Neurotensin(8-13)(Synonyms: 神经降压素(8-13))

Neurotensin(8-13) (Synonyms: 神经降压素(8-13)) 纯度: ≥98.0%

Neurotensin (8-13) 是神经降压素的活性片段,Neurotensin (8-13) 降低细胞表面NT1受体 (NTR1) 密度。

Neurotensin(8-13) (Synonyms: 神经降压素(8-13))

Neurotensin(8-13) Chemical Structure

CAS No. : 60482-95-3

规格 价格 是否有货 数量
1 mg ¥600 In-stock
5 mg ¥1200 In-stock
10 mg ¥2100 In-stock
25 mg ¥4400 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Neurotensin(8-13) 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Peptidomimetic Library
  • Peptide Library

生物活性

Neurotensin (8-13) is an active fragment of Neurotensin. Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density.

IC50 & Target

NTR1[1]

体外研究
(In Vitro)

Receptor internalization induced by Neurotensin(8-13) results in a decrease in cell-surface NT1 receptors (NTR1) density. The receptor downregulation in response to high extracellular concentrations of the peptide has been described for Neurotensin (NT) in HT-29 cells and in rat primary cultured neurons. Reappearance of the receptors on the cell surface is also different[1].

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

分子量

816.99

Formula

C38H64N12O8

CAS 号

60482-95-3

Sequence

Arg-Arg-Pro-Tyr-Ile-Leu

Sequence Shortening

RRPYIL

中文名称

神经降压素(8-13)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

H2O : 50 mg/mL (61.20 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2240 mL 6.1200 mL 12.2401 mL
5 mM 0.2448 mL 1.2240 mL 2.4480 mL
10 mM 0.1224 mL 0.6120 mL 1.2240 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 (protect from light)。-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]. García-Garayoa E, et al. Preclinical evaluation of a new, stabilized neurotensin(8–13) pseudopeptide radiolabeled with (99m)tc. J Nucl Med. 2002 Mar;43(3):374-83.

Kinase Assay
[1]

Binding assays are performed on whole HT-29 cells at confluence. A day before the assay, cells (106 cells/0.4 mL, equivalent to 0.3 mg protein) are placed in 48-well plates. A special binding buffer that includes protease inhibitors (50 mM HEPES, 125 mM NaCl, 7.5 mM KCl, 5.5 mM MgCl2, 1 mM EGTA, 5 g/L bovine serum albumin, 2 mg/L chymostatin, 100 mg/L soybean trypsin inhibitor, 50 mg/L bacitracin, pH 7.4) is used for the experiments. In inhibition studies, cells are incubated for 1 h at 37°C in triplicate with 25,000 cpm of 125I-NT and variable concentrations (0.001-3,000 nM) of unlabeled NT(8-13), unlabeled NT-VIII, or NT-VIII labeled with natRe (final volume of 0.2 mL per well). The cells are then washed twice with cold binding buffer and afterward are solubilized with 1N NaOH at 37°C (0.4 mL per well). The activity is determined in a γ-counter. In saturation studies, cells are incubated in triplicate with increasing concentrations (0.1-10 nM) of 99mTc(CO)3NT-VIII for 1 h at 37°C (final volume, 0.2 mL per well). The concentrations of total technetium (99+99mTc) are equivalent to 0.2-20 MBq 99mTc activity per well. After 2 washings with the same binding buffer as before, the cells are then solubilized with 1N NaOH at 37°C (0.4 mL per well). The bound radioactivity is measured in the γ-counter. Nonspecific binding is determined with 1 μM unlabeled NT(8-13)[1].

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

参考文献
  • [1]. García-Garayoa E, et al. Preclinical evaluation of a new, stabilized neurotensin(8–13) pseudopeptide radiolabeled with (99m)tc. J Nucl Med. 2002 Mar;43(3):374-83.

  • [1]. García-Garayoa E, et al. Preclinical evaluation of a new, stabilized neurotensin(8–13) pseudopeptide radiolabeled with (99m)tc. J Nucl Med. 2002 Mar;43(3):374-83.