Retatrutide 2381089-83-2 99+% Peptide

Not For Human Use, Lab Use Only.

Retatrutide (LY3437943) is a triple agonist peptide that targets the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM respectively.

Retatrutide( LY3437943) Cas No: 2381089-83-2 | GCGR/GIPR/GLP-1R Agonist | Kirkpeptide,.Ltd

Product Name Retatrutide
IUPAC name L-tyrosyl-2-methylalanyl-L-glutaminylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha -aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methyl-L-leucyl-Lleucyl-L-alpha -aspartyl-L-lysyl-N6-(N-(19-carboxy-1-oxononadecyl)-L-gamma-glutamyl-2-(2-(2-aminoethoxy)ethoxy)acetyl)-L-lysyl-L-alanyl-L-glutaminyl-2-methylalanyl-L-alanyl-Lphenylalanyl-L-isoleucyl-L-alpha -glutamyl-L-tyrosyl-L-leucyl-L-leucyl-L-alpha -glutamylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide
Cas No. 2381089-83-2
Synonyms LY3437943;GIPR/GLP-1R;Retatrutide;Retaglutide;Retatrutide acetate;LY3437943Retatrutide;Retatrutide/LY3437943/GIPR/GLP-1R
CBNumber: CB912574543
UNII NOP2Y096GV
ChEMBL ChEMBL5095485
Purity 99.00%
Properties State White Powder
Molecular Weight 4731.33 g/mol
Molecular Formula C221H342N46O68
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
Elemental Analysis C, 56.05; H, 7.23; N, 13.61; O, 22.99
IC50 & Target EC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R) .
EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R) .
Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1R) .
Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R).
Biological &Activity Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity。
Target: LY3437943 is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). LY3437943 inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. LY3437943 can be used for the research of obesity
In Vivo: 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]. LY3437943 (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]. LY3437943 has safety and tolerability[1]. Animal Model: Male CD-1 mice[1] Dosage: 0.47 mg/kg Administration: Subcutaneous administration, single Result: AUClast, ng*h/mL AUC0-∞, ng*h/mL Cmax, ng/mL Tmax, h t1/2, 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.
In Vitro: LY3437943 has inhibition for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively[1]. LY3437943 has inhibition for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively[1]. LY3437943 has binding affinity for human GCGR, GIPR, and GLP-1R with Ki values of 5.6, 0.057 and 7.2 nM, respectively[1]. LY3437943 has binding affinity for mouse GCGR, GIPR, and GLP-1R with Ki values of 73, 2.8 and 1.3 nM, respectively.
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Storage Condition Dry, dark and at 0 – 4 0C for short term (days to weeks) or -20 0C for long term (months to years).
Solubility H2O : 33.33 mg/mL (7.04 mM; ultrasonic and adjust pH to 7 with NaOH)
Shelf Life >2 years if stored properly
Drug Formulation This drug may be formulated in DMSO
Stock Solution Storage Sealed storage, away from moisture
Shipping Condition Shipped under ambient temperature as non-hazardous chemical.
HS Tariff Code 2934.99.9001

Description

Retatrutide is an investigational single molecule that activates the body’s receptors for three hormones – glucagon, glucose-dependent insulinotropic polypeptide (GIP), and glucagon-likepeptide-1 (GLP-1), and is being studied for the treatment of obesity. Retatrutide (LY-3437943) is an experimental drug for obesity developed by American pharmaceutical company Eli Lilly and Company. It is a triple hormone receptor agonist of GLP-1, GIP, and GCGR receptors. Our groundbreaking drug is proven to reduce weight by over 24% in non-diabetic adults battling with pre-obesity or obesity. Backed by the results of a Phase 2 trial, the drug is a peptide bearing the amino acid sequence YA1QGTFTSDYSIL2LDKK4AQA1AFIEYLLEGGPSSGAPPPS3.Our scientific breakthrough signals a new hope for effective weight management.

Mechanism of Action

Explore Retatrutide (LY3437943), an innovative triple agonist peptide targeting glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Characterized by its potent inhibition for human GCGR, GIPR, and GLP-1R with respective EC50 values of 5.79, 0.0643 and 0.775 nM, Retatrutide emerges as a significant compound in obesity research.[1].

Side effects

The most common side effects of retatrutide are gastrointestinal, including: Nausea, Diarrhea, Vomiting, and Constipation. At higher doses, researchers stated these symptoms were “mostly mild to moderate in severity” and typically treated by lowering the dosage. However, 7% of patients also experienced skin tingling. At 24 weeks of treatment, patients’ heart rates on higher doses peaked but declined afterward.

References

  • [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.
  • https://en.wikipedia.org/wiki/Retatrutide

Product Quote Form
Please enable JavaScript in your browser to complete this form.
Name
Email