Retatrutide

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Retatrutide

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2381089-83-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

LY3437943

产品介绍

Retatrutide (LY3437943) 是胰高血糖素受体(GCGR)、葡萄糖依赖性促胰岛素多肽受体(GIPR)和胰高血糖素样肽-1 受体(GLP-1R)的三重激动剂肽。Retatrutide 抑制人 GCGR、GIPR 和 GLP-1R，EC₅₀值分别为 5.79、0.0643 和 0.775 nM。Retatrutide 可用于肥胖的研究。

生物活性

Retatrutide (LY3437943) is a triple agonist peptide oftheglucagon receptor(GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide inhibits for humanGCGR, GIPR, and GLP-1R withEC₅₀values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity^[1].

IC₅₀& Target

EC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R)^[1].
EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R)^[1].
Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1R)^[1].
Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R)^[1].

体外研究
(In Vitro)

Retatrutide (LY3437943) has inhibition for human GCGR, GIPR, and GLP-1R with EC₅₀values of 5.79, 0.0643 and 0.775 nM, respectively^[1].
Retatrutide has inhibition for mouse GCGR, GIPR, and GLP-1R with EC₅₀values of 2.32, 0.191 and 0.794 nM, respectively^[1].
Retatrutide has binding affinity for human GCGR, GIPR, and GLP-1R with K_ivalues of 5.6, 0.057 and 7.2 nM, respectively^[1].
Retatrutide has binding affinity for mouse GCGR, GIPR, and GLP-1R with K_ivalues of 73, 2.8 and 1.3 nM, respectively^[1].

体内研究
(In Vivo)

Retatrutide (LY3437943) (s.c.; 0.47 mg/kg; single) engages GCGR in vivo and can improve glucose tolerance in an ipGTT through either the GIP or GLP-1 receptors^[1].
Retatrutide (s.c.; 10 mL/kg; cycle every 3 days; for 21 days) causes great body weight loss and increases energy expenditure through glucagon receptor activatio^[1].
Retatrutide has safety and tolerability^[1].

Animal Model:

Male CD-1 mice^[1]

Dosage:

0.47 mg/kg

Administration:

Subcutaneous administration, single

Result:

AUC_last, ng*h/mL	AUC_0-∞, ng*h/mL	C_max, ng/mL	T_max, h	t_1/2, h	CLF, mL/h/kg
41135	41905	1680	12	21	11.22

Animal Model:	Diet-induced obese (DIO) male C57/Bl6 mice (24-25 weeks, 40-51 g)^[1]
Dosage:	10 mL/kg
Administration:	Subcutaneous (SC) injection, cycle every 3 days, for 21 days
Result:	Decreased body weight and improved glycemic control.

Clinical Trial

分子量

4731.33

Formula

C₂₂₁H₃₄₂N₄₆O₆₈

CAS 号

2381089-83-2

Sequence

Tyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{α-Me-Leu}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(AEEA)-Lys}-Ala-Gln-{Aib}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-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.