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Retatrutide

Catalog No. T76279 CAS 2381089-83-2

Synonyms: LY3437943

Retatrutide (LY3437943) is a triple agonist of the glucagon receptor, glucose-dependent insulinotropic polypeptide receptor, and glucagon-like peptide-1 receptor (GLP-1R), and inhibits GCGR, GIPR, and GLP-1R.Retatrutide can be used to study obesity.

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Retatrutide, CAS 2381089-83-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 247.00
5 mg	In stock	$ 622.00
10 mg	In stock	$ 997.00
25 mg	In stock	$ 1,470.00
50 mg	In stock	$ 1,990.00
100 mg	In stock	$ 2,690.00

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Purity: 98.31%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Retatrutide (LY3437943) is a triple agonist of the glucagon receptor, glucose-dependent insulinotropic polypeptide receptor, and glucagon-like peptide-1 receptor (GLP-1R), and inhibits GCGR, GIPR, and GLP-1R.Retatrutide can be used to study obesity.
Targets&IC50	GIPR:0.0643 nM (EC50, human), GIPR:0.057 nM (Ki, human), GLP1R:0.794 nM (EC50, mouse), GIPR:2.8 nM (Ki, mouse), GCGR:5.79 nM (EC50, human), GCGR:2.32 nM (EC50, mouse), GCGR:73 nM (Ki, mouse), GLP1R:7.2 nM (Ki, human), GIPR:0.191 nM (EC50, mouse), GLP1R:1.3 nM (Ki, mouse), GCGR:5.6 nM (Ki, human), GLP1R:0.775 nM (EC50, human)
In vitro	Retatrutide (LY3437943) exhibits activity against human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM, respectively[1]. For mouse GCGR, GIPR, and GLP-1R, Retatrutide shows activity with EC50 values of 2.32, 0.191, and 0.794 nM, respectively[1]. In terms of binding affinity, Retatrutide has Ki values of 5.6, 0.057, and 7.2 nM for human GCGR, GIPR, and GLP-1R, respectively[1]. Similarly, for mouse GCGR, GIPR, and GLP-1R, Retatrutide exhibits binding affinity with Ki values of 73, 2.8, and 1.3 nM, respectively[1].
In vivo	In vivo, Retatrutide (LY3437943) engages with GCGR and, when administered through subcutaneous injection at a single dose of 0.47 mg/kg, improves glucose tolerance in an ipGTT (intraperitoneal glucose tolerance test) through activation of GIP or GLP-1 receptors[1]. With subcutaneous injections at 10 mL/kg every 3 days in a cycle sustained for 21 days, Retatrutide leads to significant weight reduction and increased energy expenditure through activation of glucagon receptor[1].

Synonyms	LY3437943
Molecular Weight	4731.33
Formula	C221H342N46O68
CAS No.	2381089-83-2

Storage

store at low temperature,keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 30 mg/mL (6.34 mM), when pH is adjusted to 7 with NaOH. Sonication is recommended.

DMSO: 30 mg/mL (6.34 mM), Sonication is recommended.

References and Literature

1. Tamer Coskun, et al. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.

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Keywords

Retatrutide 2381089-83-2 GPCR/G Protein Glucagon Receptor LY3437943 inhibitor inhibit

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