HOME
NETWORK
CONTACT US
 
¡¡Products
  Peptide
GLP-1 / GIP Retatrut (2381089-83-2)
 
Detailed Description
Name: Retatrutide
Synonyms: LY3437943; GIPR/GLP-1R; Retatrutide/LY3437943/GIPR/GLP-1R

CAS Registry number: 2381089-83-2


Retatrutide (LY-3437943) is an experimental drug for obesity . It is a triple hormone receptor agonist of GLP-1, GIP, and GCGR receptors. It has been shown to achieve a more than 24% mean weight reduction in non-diabetic obese or overweight adults during a phase 2 trial. The drug is a peptide with amino acid sequence YA1QGTFTSDYSIL2LDKK4AQA1AFIEYLLEGGPSSGAPPPS3.

Clinical data
Other names LY-3437943
Identifiers

CAS Number
  • 2381089-83-2
UNII
  • NOP2Y096GV
ChEMBL
  • ChEMBL5095485
Chemical and physical data
Formula C223H343F3N46O70
Molar mass 4845.444 g¡¤mol?1


Description 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[1].
Related Catalog Research Areas >> Metabolic Disease
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 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[1].
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-¡Ş, 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.


Appearance: Powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 
 
Shanghai Getian Industrial Co.,Ltd. is a professional company engaged in health care products, cosmetics raw materials,
with rich experience and high-quality talent team. We are committed to providing customers with quality, efficient and professional services to help customers realize their dreams.Our company has a good reputation in the industry, thanks to our professional team...
 
Copyright © 2024 Shanghai Getian Industrial Co.,Ltd. All rights reserved