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PX-102

Cat. No. M6157
PX-102 Structure
Synonym:

PX20606

Size Price Availability
1mg USD 133  USD133 Custom Synthesis
5mg USD 443  USD443 Custom Synthesis
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Quality Control & Documentation
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 (for reference only)
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
Chemical Information
Molecular Weight 554.85
Formula C29H22Cl3NO4
CAS Number 1268244-85-4
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Schwabl P, et al. J Hepatol. The FXR agonist PX20606 ameliorates portal hypertension by targeting vascular remodelling and sinusoidal dysfunction.

[2] Hambruch E, et al. J Pharmacol Exp Ther. 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.

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Keywords: PX-102, PX20606 supplier, Farnesoid X Receptor, inhibitors, activators


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