Beschreibung
Retatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values 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]. In Vitro
Retatrutide (LY3437943) has efficacy for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively[1]. Retatrutide has efficacy for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively[1]. Retatrutide has binding affinity for human GCGR, GIPR, and GLP-1R with Ki values of 5.6, 0.057 and 7.2 nM, respectively[1]. Retatrutide has binding affinity for mouse GCGR, GIPR, and GLP-1R with Ki values of 73, 2.8 and 1.3 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo
Retatrutide (LY3437943) (s.c.; 47 μg/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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male CD-1 mice[1] Dosage: 47 μg/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. Molekulargewicht
4731.33 Formel
C221H342N46O68 CAS. Nr.
2381089-83-2 Appearance
Solid Color
White to off-white 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 Sequence Shortening
Y-{Aib}-QGTFTSDYSI-{α-Me-Leu}-LDK-{Lys(AEEA-γGlu-C20 diacid)}AQ-{Aib}-AFIEYLLEGGPSSGAPPPS-NH2 Versand
Room temperature in continental US; may vary elsewhere. Speicherung
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (10.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 20 mg/mL (4.23 mM; ultrasonic and adjust pH to 9 with NH3·H2O)
Preparing Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2114 mL 1.0568 mL 2.1136 mL 5 mM 0.0423 mL 0.2114 mL 0.4227 mL
View the Complete Stock Solution Preparation Table
* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Molaritätsrechner
Verdünnungsrechner
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Mass
= Concentration
× Volume
× Molecular Weight *
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 Concentration (start)
C1
× Volume (start)
V1
= Concentration (final)
C2
× Volume (final)
V2
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE). Reinheit & Dokumentation
Purity: 99.96%
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SDS (252 KB)
COA (273 KB) RP-HPLC (263 KB) MS (69 KB)
Handling Instructions (2659 KB) Verweise
[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. [Content Brief]