SB-756050
SB-756050 Basic information
- Product Name:
- SB-756050
- Synonyms:
-
- SB-756050
- 1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane
- SB756050;SB 756050;SB-756050
- SB-756050, >98%
- 1H-1,4-Diazepine, 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]hexahydro-
- G protein-coupled Bile Acid Receptor 1,inhibit,TGR5,Inhibitor,SB756050,GPBAR1,G-protein coupled receptor 19,GPCR19
- SB756050, 10 mM in DMSO
- SB-756050 ，S6741
- CAS:
- 447410-57-3
- MF:
- C21H28N2O8S2
- MW:
- 500.59
- Mol File:
- 447410-57-3.mol
SB-756050 Chemical Properties
- Boiling point:
- 653.1±65.0 °C(Predicted)
- Density
- 1.328±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMF: 10 mg/ml; DMF:PBS (pH 7.2) (1:2): 0.25 mg/ml; DMSO: 10 mg/ml
- form
- A crystalline solid
- pka
- -6.97±0.20(Predicted)
- color
- White to off-white
SB-756050 Usage And Synthesis
Description
SB-756050 is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50 = 1.3 μM for the human receptor). It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters. SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats.
Uses
SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
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 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. DOI:10.1002/cpdd.34
SB-756050Supplier
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- 13621943973
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