Tropifexor - CAS 1383816-29-2
Catalog number: B0084-008115
Category: Inhibitor
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Molecular Formula:
C29H25F4N3O5S
Molecular Weight:
603.589
COA:
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Targets:
FXR
Description:
Tropifexor is a novel highly potent agonist of farnesoid X receptor (FXR), which regulates bile acid metabolism and signaling. FXR activated by Tropifexor can inhibit bile acid synthesis as well as increase bile acid conjugation, transport and excretion. Tropifexor entered phase II clinical trials for the treatment of NASH and PBC.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-008115 10 mg $198 In stock
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Brife Description:
FXR agonist
Purity:
≥98%
Appearance:
Solid powder
Synonyms:
LJN-452; 2-[(1R,5S)-3-[[5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl]methoxy]-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylic acid
Solubility:
Soluble in DMSO
MSDS:
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InChIKey:
VYLOOGHLKSNNEK-JWTNVVGKSA-N
InChI:
InChI=1S/C29H25F4N3O5S/c30-21-9-15(27(37)38)10-23-25(21)34-28(42-23)36-16-7-8-17(36)12-18(11-16)39-13-20-24(35-41-26(20)14-5-6-14)19-3-1-2-4-22(19)40-29(31,32)33/h1-4,9-10,14,16-18H,5-8,11-13H2,(H,37,38)/t16-,17+,18?
Canonical SMILES:
C1CC1C2=C(C(=NO2)C3=CC=CC=C3OC(F)(F)F)COC4CC5CCC(C4)N5C6=NC7=C(C=C(C=C7S6)C(=O)O)F
1.Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Tully DC;Rucker PV;Chianelli D;Williams J;Vidal A;Alper PB;Mutnick D;Bursulaya B;Schmeits J;Wu X;Bao D;Zoll J;Kim Y;Groessl T;McNamara P;Seidel HM;Molteni V;Liu B;Phimister A;Joseph SB;Laffitte B J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8.
The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases bile acid conjugation, transport, and excretion, thereby protecting the liver from the harmful effects of bile accumulation, leading to considerable interest in FXR as a therapeutic target for the treatment of cholestasis and nonalcoholic steatohepatitis. We identified a novel series of highly potent non-bile acid FXR agonists that introduce a bicyclic nortropine-substituted benzothiazole carboxylic acid moiety onto a trisubstituted isoxazole scaffold. Herein, we report the discovery of 1 (tropifexor, LJN452), a novel and highly potent agonist of FXR. Potent in vivo activity was demonstrated in rodent PD models by measuring the induction of FXR target genes in various tissues. Tropifexor has advanced into phase 2 human clinical trials in patients with NASH and PBC.
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