SB756050

Modify Date: 2024-01-22 22:56:44

SB756050 Structure
SB756050 structure
Common Name SB756050
CAS Number 447410-57-3 Molecular Weight 500.586
Density 1.3±0.1 g/cm3 Boiling Point 653.1±65.0 °C at 760 mmHg
Molecular Formula C21H28N2O8S2 Melting Point N/A
MSDS N/A Flash Point 348.8±34.3 °C

 Use of SB756050


SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.

 Names

Name SB756050
Synonym More Synonyms

 SB756050 Biological Activity

Description SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
Related Catalog
In Vitro TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D)[1].
In Vivo SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 þ sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different[1].
References

[1]. Hodge RJ, et al. Safety, Pharmacokinetics, and Pharmacodynamic Effects of a Selective TGR5 Agonist, SB-756050, in Type 2 Diabetes. Clin Pharmacol Drug Dev. 2013 Jul;2(3):213-22.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 653.1±65.0 °C at 760 mmHg
Molecular Formula C21H28N2O8S2
Molecular Weight 500.586
Flash Point 348.8±34.3 °C
Exact Mass 500.128693
LogP 4.70
Appearance of Characters white solid
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.569

 Synonyms

MFCD02585318
1H-1,4-Diazepine, 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]hexahydro-
1,4-Bis[(3,4-dimethoxyphenyl)sulfonyl]-1,4-diazepane
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