Details
Stereochemistry | RACEMIC |
Molecular Formula | C29H22Cl3NO4 |
Molecular Weight | 554.848 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)C1=CC=C(C=C1)[C@H]2C[C@@H]2C3=CC=C(OCC4=C(ON=C4C5=C(Cl)C=CC=C5Cl)C6CC6)C=C3Cl
InChI
InChIKey=XBUXXJUEBFDQHD-NHCUHLMSSA-N
InChI=1S/C29H22Cl3NO4/c30-23-2-1-3-24(31)26(23)27-22(28(37-33-27)16-6-7-16)14-36-18-10-11-19(25(32)12-18)21-13-20(21)15-4-8-17(9-5-15)29(34)35/h1-5,8-12,16,20-21H,6-7,13-14H2,(H,34,35)/t20-,21-/m1/s1
PX-102 is a methoxyphenylcyclopropane derivative patented by Phenex Pharmaceuticals AG as Farnesoid X receptor agonists useful in the treatment and prophylaxis of FXR-mediated diseases. The Farnesoid X Receptor (FXR) is a bile acid receptor which when activated by Px-102 has a profound positive impact on cholesterol, triglyceride and glucose metabolism in liver and intestine. In preclinical studies, Px-102 potently reduces intestinal uptake of neutral lipids and cholesterol and at the same time enhances the excretion of these lipid species. In addition, Px-102 improves hepatic insulin sensitivity and shows massive hepatoprotective effects in animal models of liver cirrhosis or fibrosis. Phenex Pharmaceuticals completes a phase I trial in Healthy volunteers in Germany in 2012 and no further development report has been published.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29928896
0.15 mg/kg, 0.3 mg/kg, 0.6 mg/kg, 1.12 mg/kg, 2.25 mg/kg, 3.38 mg/kg, or 4.5 mg/kg
Route of Administration:
Oral
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1268244-85-4
Created by
admin on Sat Dec 16 11:43:26 GMT 2023 , Edited by admin on Sat Dec 16 11:43:26 GMT 2023
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CHEMBL3545113
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admin on Sat Dec 16 11:43:26 GMT 2023 , Edited by admin on Sat Dec 16 11:43:26 GMT 2023
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PX-20606
Created by
admin on Sat Dec 16 11:43:26 GMT 2023 , Edited by admin on Sat Dec 16 11:43:26 GMT 2023
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PRIMARY | MedKoo CAT NO: 522554, CAS NO: 1268245-19-7(free acid)Description: PX20606, also known as PX-102, is a FXR agonist. PX20606 induces high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice. PX20606 demonstrated potent plasma cholesterol-lowering activity that affected all lipoprotein species. (last updated: 3/21/2016). | ||
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1268245-19-7
Created by
admin on Sat Dec 16 11:43:26 GMT 2023 , Edited by admin on Sat Dec 16 11:43:26 GMT 2023
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6TU6SUZ3BY
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118374999
Created by
admin on Sat Dec 16 11:43:26 GMT 2023 , Edited by admin on Sat Dec 16 11:43:26 GMT 2023
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ACTIVE MOIETY