Z-Guggulsterone is a mineralocorticoid, progesterone and glucocorticoid receptor antagonist (Ki values are 37, 224 and 252 nM respectively) and weak androgen receptor agonist (Ki = 315 nM). Z-Guggulsterone induces apoptosis in prostate cancer cells and inhibits angiogenesis via suppression of the VEGF-VEGFR2-Akt signaling pathway. Z-Guggulsterone exhibits antilipidemic activity via antagonism of the farnesoid X receptor (FXR) and displays antiseptic, antirheumatic and anti-inflammatory activity in vivo.
|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||DMSO 20 mM (with gentle warming)|
z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo.
Xiao D, et al. Mol Cancer Ther. 2008 Jan;7(1):171-80. PMID: 18202020.
Guggulsterone-induced apoptosis in human prostate cancer cells is caused by reactive oxygen intermediate dependent activation of c-Jun NH2-terminal kinase.
Singh SV, et al. Cancer Res. 2007 Aug 1;67(15):7439-49. PMID: 17671214.
|Related Farnesoid X Receptor Products|
DY268 is a potent FXR antagonist with IC50 of 7.5 nM.
Nidufexor is a farnesoid X receptor (FXR) agonist.
Cilofexor is a farnesoid X receptor (FXR) agonist.
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.
Tropifexor is a novel and highly potent agonist of farnesoid X receptor (FXR).
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