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PX-102

Cat. No. M6157
PX-102 Structure
Synonym:

PX20606

Size Price Availability
1mg USD 120 Custom Synthesis
5mg USD 320 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PX-102, also known as PX20606, is a FXR agonist. PX-102 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. PX-102 demonstrated potent plasma cholesterol-lowering activity that affected all lipoprotein species.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models LDLR(−/−) mice
Formulation 21% milk fat and 0.15% cholesterol
Dosages 5 or 25 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 554.85
Formula C29H22Cl3NO4
CAS Number 1268244-85-4
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

The FXR agonist PX20606 ameliorates portal hypertension by targeting vascular remodelling and sinusoidal dysfunction.
Schwabl P, et al. J Hepatol. 2017 Apr;66(4):724-733. PMID: 27993716.

Synthetic farnesoid X receptor agonists induce 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.
Hambruch E, et al. J Pharmacol Exp Ther. 2012 Dec;343(3):556-67. PMID: 22918042.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PX-102, PX20606 supplier, inhibitors

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