SBI-115|TGR5 (GPCR19) antagonist|cas 882366-16-7

Cas No.:	882366-16-7
Chemical Name:	4-Pyrimidinecarboxylic acid, 5-chloro-2-(ethylsulfonyl)-, 3-methylphenyl ester
Synonyms:	SBI-115; SBI 115; SBI115
SMILES:	O=C(C1=NC(S(=O)(CC)=O)=NC=C1Cl)OC2=CC=CC(C)=C2
Formula:	C₁₄H₁₃ClN₂O₄S
M.Wt:	340.02
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibitingTGR5[1].
In Vitro:	SBI-115 (100 and 200 µM, 24 hours) inhibits proliferation triggered by pre-treatment of cystic cholangiocytes with Taurolithocholic acid (TLCA) in shRNA-transfected ADPKD cholangiocytes[1]. Cell Proliferation Assay[1] Cell Line: shRNA-transfected ADPKD cholangiocytes Concentration: 100 and 200 µM Incubation Time: 24 hours Result: Inhibited proliferation (by 32-48%) triggered by pre-treatment of cystic cholangiocytes with TLCA.
References:	[1]. Masyuk TV, et al. TGR5 contributes to hepatic cystogenesis in rodents with polycystic liver diseases through cyclic adenosine monophosphate/Gαs signaling. Hepatology. 2017 Oct; 66(4):1197-1218.

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