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SB756050

  Cat. No.:  DC10470   Featured
Chemical Structure
447410-57-3
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More than 5000 active chemicals with high quality for research!
Field of application
SB-756050 is a Farnesoid X receptor (FXR) (NR1H4) agonist.
Cas No.: 447410-57-3
Chemical Name: 1H-1,4-Diazepine, 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]hexahydro-
Synonyms: SB756050,SB 756050,SB-756050
SMILES: COC1=C(C=C(C=C1)S(=O)(=O)N2CCCN(CC2)S(=O)(=O)C3=CC(=C(C=C3)OC)OC)OC
Formula: C21H28N2O8S2
M.Wt: 500.59
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SB756050 is a selective TGR5 agonist currently in phase 1clinical trials for the treatment of type 2 diabetes.
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 t sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different[1].
In Vitro: TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D)[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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC71956 BMS-986339 BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues.
DC7040 WAY-362450 (XL335; Turofexorate isopropyl) WAY-362450 (XL335; Turofexorate isopropyl) is a highly potent, selective, and orally active farnesoid X receptor (FXR) agonist with an EC50 of 4 nM.WAY-362450 is useful for dyslipidemia.
DC10737 Tropifexor (LJN452) Tropifexor (LJN452) is a highly potent non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
DC10470 SB756050 SB-756050 is a Farnesoid X receptor (FXR) (NR1H4) agonist.
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