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.
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Retatrutide (LY3437943) Cas No: 2381089-83-2 | GCGR/GIPR/GLP-1R Agonist | 99%+ | Kirkpeptide,.Ltd
Buy Retatrutide Online | all in one tube
| 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). |
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| 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. |
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| 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].
Medical Usage
- treating type 2 diabetes
- treating obesity
- for now, it’s not approved by FDA yet, but it’s in phase 3 clinical trial, we can expect it to be approved soon
- safety of retatrutide is very good
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
Categories: GLP-1 Receptor Agonists, Popular Peptide
Tags: GLP-1 Receptor Agonist
