SB756050

Names

[ Name ]:
SB756050

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

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> GPCR19

Research Areas >> Metabolic Disease

[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.

[Related Small Molecules]

INT-777 | INT-767 | Deoxycholic acid | BAR501 | TGR5 | BAR502 | Hyodeoxycholic acid

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