G-Protein antagonist peptide

G-Protein antagonist peptide;

G-Protein antagonist peptide 是一种 substance P 相关肽,可抑制 G 蛋白与其受体的结合。G-Protein antagonist peptide 竞争性和可逆性地抑制毒蕈碱型乙酰胆碱受体 M2 (M2 muscarinic receptor) 对 Gi 或 Go 的激活,并通过 β-肾上腺素受体抑制 Gs 的激活。

G-Protein antagonist peptideamp;;

G-Protein antagonist peptide Chemical Structure

CAS No. : 143675-79-0

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

* Please select Quantity before adding items.

生物活性

G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

分子量

1093.26

Formula

C5H7FN2O2W3

CAS 号

143675-79-0

Sequence

{Glp}-Gln-Trp-Phe-Trp-Trp-Met-NH2

Sequence Shortening

{Glp}QWFWWM-NH2

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]. Mukai H, et al. G protein antagonists. A novel hydrophobic peptide competes with receptor for G protein binding. J Biol Chem. 1992;267(23):16237-16243.

CXCR4 antagonist 4

CXCR4 antagonist 4;

CXCR4 antagonist 4 是一种有效,具有口服活性的 CXCR4 拮抗剂 (IC50=24 nM),可降低 CYP 2D6 的活性,提高 PAMPA 的通透性,有效抑制人类免疫缺陷病毒的进入 (IC50=7 nM).

CXCR4 antagonist 4amp;;

CXCR4 antagonist 4 Chemical Structure

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

* Please select Quantity before adding items.

生物活性

CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM)[1].

IC50 Target

CXCR4

24 nM (IC50)

HIV

7 nM (IC50)

体外研究
(In Vitro)

CXCR4 antagonist 4 (Compound 30, 0.1~10 µM, 48 hours) displays the inhibition potencies against the X4 virus in TZM-bl cells (IC50=7 nM) [1].

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

Cell Cytotoxicity Assay[1]

Cell Line: TZM-bl cells
Concentration: 0.1, 1, 10 µM
Incubation Time: 48 hours
Result: Displayed inhibition potencies against the X4 virus (IC50=7 nM)

体内研究
(In Vivo)

CXCR4 antagonist 4 (3, 10, 30 mg/kg) demonstrates better oral Bioavailability in a dose dependent and reached 27% for the 30 mg/kg[1]. Pharmacokinetic Parameters of CXCR4 antagonist 4 in mice[1]

Route Dose(mg/kg) T1/2(h) Cmax(ng/mL) C12h (ng/mL) AUC0-8h(h*ng/mL) % FPO (0-8 h) Cl (L/h/kg) Vd (L/kg)
iv 3 5.89 116 265 11.3 96.3
po 3 12.8 1.50 34.3 12.9
po 10 54.8 14.3 190 215
po 30 169 34.8 717 27.1

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

Animal Model: mice[1]
Dosage: 3, 10, 30 mg/kg
Administration:
Result: Demonstrated better oral bioavailability in a dose dependent and reached 27% for the 30 mg/kg.

分子量

497.67

Formula

C29H41F2N5

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]. Jecs E, et al. Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles. J Med Chem. 2022, 65(5):4058-4084.

Antagonist G TFA

Antagonist G TFA;

Antagonist G TFA 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录,是癌细胞对化疗增敏。

Antagonist G TFAamp;;

Antagonist G TFA Chemical Structure

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

* Please select Quantity before adding items.

Antagonist G TFA 的其他形式现货产品:

Antagonist G

生物活性

Antagonist G TFA is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].

体外研究
(In Vitro)

Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2].
Antagonist G activates JNK1 in SCLC cells[2].
Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[2].

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

Cell Viability Assay[2]

Cell Line: SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
Concentration: 0-100 μM.
Incubation Time: 24 h.
Result: Inhibited cell growh.

分子量

1065.21

Formula

C51H67F3N12O8S

Sequence Shortening

RW-{Me-Phe}-WLM-NH2

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]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.

    [2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.

RAGE antagonist peptide

RAGE antagonist peptide;

RAGE antagonist peptide 是一种晚期糖基化终产物 (RAGE) 拮抗剂。RAGE antagonist peptide (RAP) 可阻断 RAGE 和几个重要配体 HMGB-1、S100P、S100A4 的结合。RAGE antagonist peptide (RAP) 具有抗肿瘤和抗炎活性。

RAGE antagonist peptideamp;;

RAGE antagonist peptide Chemical Structure

CAS No. : 1092460-91-7

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

* Please select Quantity before adding items.

RAGE antagonist peptide 的其他形式现货产品:

RAGE antagonist peptide TFA

生物活性

RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities[1][2].

体外研究
(In Vitro)

RAGE antagonist peptide (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro[1].

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

体内研究
(In Vivo)

RAGE antagonist peptide (RAP, 100 µg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[1].
RAGE antagonist peptide (RAP) reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth[1].
In mice bearing asthma, RAGE antagonist peptide (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide also reduces total, cytoplasmic and nuclear levels of β-catenin, enhanced β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[2].

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

Animal Model: Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Dosage: 100 µg.
Administration: Intratumoral delivery (or intraperitoneally).
Result: Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection.

分子量

1272.56

Formula

C57H101N13O17S

CAS 号

1092460-91-7

Sequence Shortening

Ac-ELKVLMEKEL-NH2

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]. Thiruvengadam Arumugam, et al. S100P-derived RAGE antagonistic peptide reduces tumor growth and metastasis. Clin Cancer Res. 2012 Aug 15;18(16):4356-64.

    [2]. Lihong Yao, et al. The receptor for advanced glycation end products is required for β-catenin stabilization in a chemical-induced asthma model. Br J Pharmacol. 2016 Sep;173(17):2600-13.

RAGE antagonist peptide TFA

RAGE antagonist peptide TFA; 纯度: 99.04%

RAGE antagonist peptide TFA 是一种晚期糖基化终产物 (RAGE) 拮抗剂。RAGE antagonist peptide TFA 可阻断 RAGE 和几个重要配体 HMGB-1,S100P,S100A4 的结合。RAGE antagonist peptide TFA 具有抗肿瘤和抗炎活性。

RAGE antagonist peptide TFAamp;;

RAGE antagonist peptide TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥890 In-stock
5 mg ¥2700 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

RAGE antagonist peptide TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Peptide Library

生物活性

RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities[1][2].

体外研究
(In Vitro)

RAGE antagonist peptide TFA (RAP) reduces the ability of the ligands to stimulate RAGE activation of NFκB in cancer cells in vitro[1].

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

体内研究
(In Vivo)

RAGE antagonist peptide TFA (RAP, 100 µg) inhibits RAGE-mediated Basal NFκB Activity in PDAC cells in vivo[1].
RAGE antagonist peptide TFA (RAP) reduces the growth and metastasis of pancreatic tumors and also inhibited glioma tumor growth[1].
In mice bearing asthma, RAGE antagonist peptide TFA (RAP; 4 mg/kg; i.p.) blunts airway reactivity, airway inflammation and goblet cell metaplasia, and decreases release of Th2 cytokines. RAGE antagonist peptide TFA also reduces total, cytoplasmic and nuclear levels of β-catenin, enhances β-catenin phosphorylation at Ser33/37/Thr41, which triggers ubiquitination, down-regulated expression of β-catenin targeted genes, and tends to keep β-catenin at the cytomembrane, shifting β-catenin from a signalling active pattern to an adhesive function[2].

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

Animal Model: Cancer cells expressing the NFκB-luc reporter implanted into immune-deficient mice[1].
Dosage: 100 µg
Administration: Intratumoral delivery (or intraperitoneally).
Result: Systemic administration caused a substantial reduction (p<0.05) in the NFκB signal 5 h after injection.

分子量

1386.58

Formula

C59H102F3N13O19S

Sequence Shortening

Ac-ELKVLMEKEL-NH2

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 : 25 mg/mL (18.03 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7212 mL 3.6060 mL 7.2120 mL
5 mM 0.1442 mL 0.7212 mL 1.4424 mL
10 mM 0.0721 mL 0.3606 mL 0.7212 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]. Thiruvengadam Arumugam, et al. S100P-derived RAGE antagonistic peptide reduces tumor growth and metastasis. Clin Cancer Res. 2012 Aug 15;18(16):4356-64.

    [2]. Lihong Yao, et al. The receptor for advanced glycation end products is required for β-catenin stabilization in a chemical-induced asthma model. Br J Pharmacol. 2016 Sep;173(17):2600-13.

G-Protein antagonist peptide TFA

G-Protein antagonist peptide TFA; 纯度: 97.35%

G-Protein antagonist peptide TFA 是一种截短的 substance P 相关肽,与受体竞争 G 蛋白结合。G-Protein antagonist peptide TFA 抑制重组磷脂囊泡中 M2 毒蕈碱胆碱能受体 (M2 mAChR) 激活 Gi 或 Go 或 β 肾上腺素能受体激活 Gs

G-Protein antagonist peptide TFAamp;;

G-Protein antagonist peptide TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥1500 In-stock
5 mg ¥4000 In-stock
10 mg ¥6400 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

生物活性

G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis[1].

分子量

1207.28

Formula

C59H65F3N12O11S

Sequence

{Glp}-Gln-Trp-Phe-Trp-Trp-Met-NH2

Sequence Shortening

{Glp}QWFWWM-NH2

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 : 50 mg/mL (41.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.8283 mL 4.1415 mL 8.2831 mL
5 mM 0.1657 mL 0.8283 mL 1.6566 mL
10 mM 0.0828 mL 0.4142 mL 0.8283 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 ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.07 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (2.07 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Mukai H, et al. G protein antagonists. A novel hydrophobic peptide competes with receptor for G protein binding. J Biol Chem. 1992;267(23):16237-16243.

Antagonist G

Antagonist G; 纯度: 95.0%

Antagonist G 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的 GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录,是癌细胞对化疗增敏。

Antagonist Gamp;;

Antagonist G Chemical Structure

CAS No. : 115150-59-9

规格 价格 是否有货 数量
1 mg ¥1500 In-stock
5 mg ¥4500 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

* Please select Quantity before adding items.

Antagonist G 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • GPCR/G Protein Compound Library
  • Anti-Cancer Compound Library
  • Transcription Factor Targeted Library
  • Peptide Library

生物活性

Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].

体外研究
(In Vitro)

Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2].
Antagonist G activates JNK1 in SCLC cells[2].
Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[2].

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

Cell Viability Assay[2]

Cell Line: SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
Concentration: 0-100 μM.
Incubation Time: 24 h.
Result: Inhibited cell growh.

分子量

951.19

Formula

C49H66N12O6S

CAS 号

115150-59-9

Sequence Shortening

RW-{Me-Phe}-WLM-NH2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light

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

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (protect from 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]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.

    [2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.