Retatrutide (Synonyms: LY3437943) raw material

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Retatrutide (Synonyms: LY3437943) raw material

Original price was: $28.00.Current price is: $23.00.

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.

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Description

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.

For research use only. We do not sell to patients.

Description

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.

Retatrutide Related Antibodies

  • GLP-1R Antibody
  • Glucagon Antibody
  • gamma Sarcoglycan Antibody (YA1357)
  • delta Sarcoglycan Antibody (YA3326)
In Vivo

Retatrutide (LY3437943) (s.c.; 47 g/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 g/kg
Administration:Subcutaneous administration, single
Result:
AUClast, ng*h/mLAUC0-?, ng*h/mLCmax, ng/mLTmax, ht1/2, hCLF, mL/h/kg
41135419051680122111.22
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT05931367Eli Lilly and Company
Obesity|Overweight|Osteo Arthritis Knee
August 28, 2023Phase 3
NCT05929066Eli Lilly and Company
Obesity|Overweight|Knee Pain Chronic|Knee Osteoarthritis|Obstructive Sleep Apnea
August 7, 2023Phase 3
NCT05882045Eli Lilly and Company
Obesity|Cardiovascular Diseases
May 30, 2023Phase 3
NCT05611957Eli Lilly and Company
Healthy|Renal Insufficiency
November 16, 2022Phase 1
NCT04881760Eli Lilly and Company
Obesity|Overweight
May 20, 2021Phase 2
NCT05445232Eli Lilly and Company
Obesity
July 8, 2022Phase 1
NCT04823208Eli Lilly and Company
Diabetes Mellitus, Type 2
May 24, 2021Phase 1
NCT05936151Eli Lilly and Company
Overweight or Obesity|CKD|Type 2 Diabetes
July 20, 2023Phase 2
NCT06003465Eli Lilly and Company
Healthy
August 29, 2023Phase 1
NCT05916560Eli Lilly and Company
Healthy|Hepatic Insufficiency
July 13, 2023Phase 1
NCT05929079Eli Lilly and Company
Type 2 Diabetes|Obesity|Overweight|Obstructive Sleep Apnea
July 11, 2023Phase 3
NCT05548231Eli Lilly and Company
Overweight|Obesity
October 24, 2022Phase 1
NCT04143802Eli Lilly and Company
Diabetes Mellitus, Type 2
December 18, 2019Phase 1
NCT05959096Eli Lilly and Company
Healthy
July 18, 2023Phase 1
NCT03841630Eli Lilly and Company
Healthy
March 13, 2019Phase 1
NCT04867785Eli Lilly and Company
Type 2 Diabetes
May 13, 2021Phase 2
Molecular Weight

4731.33

Formula

C221H342N46O68

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{?-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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

Powder-80°C2 years
-20°C1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

 

Additional information

Weight1 kg
Dimensions36 × 52 × 46 cm

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