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.
|Animal models||LDLR(−/−) mice|
|Formulation||21% milk fat and 0.15% cholesterol|
|Dosages||5 or 25 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||10 mM in DMSO|
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.
Disufide crosslinks of cystines in proteins can be reduced to cysteine residues by TCEP (tris-(2-carboxyethyl)phosphine). Unlike DTT (dithiothreitol), TCEP does not contain thiols and therefore usually does not need to be removed prior to thiol modification.
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
6-Chloropurine is used in the preparation of 9-alkylpurines through alkylation with various substituted alkyl halides in dimethyl sulfoxide.
Lanolin is a wax secreted by the sebaceous glands of wool-bearing animals and used widely in the pharmaceutical and cosmetics industries.
Potassium acetate is the potassium salt of acetic acid, which is a synthetic carboxylic acid with antibacterial and antifungal properties.
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