深圳欣博盛生物科技有限公司

T0901317

TO-901317; T 1317

T0901317 is a potent, cell permeable and selective agonist of LXRalpha and LXRbeta (EC50 of 50nM, Kd values are 7 and 22 nM for LXR-alpha and LXR-beta, respectively), results in LXR-dependent up-regulation of ABC1 gene expression. The Liver X Receptors (LXRalpha and LXRbeta) are nuclear hormone receptors whose native ligands are oxysterols. T0901317 acting through LXR and in concert with its RXR heterodimerization partner induces the expression of the ABCA1 reverse cholesterol transporter. This acts to increase the efflux of cholesterol and regulation of HDL metabolism. T0901317 activates farnesoid X receptor (FXR) (EC50 ~5µM), less potent then LXR, but activates FXR more potently than a natural bile acid FXR ligand, chenodeoxycholic acid. It also is a high-affinity ligand for the xenobiotic receptor pregnane X receptor (PXR). T0901317 binds and activates PXR with the same nanomolar potency with which it stimulates LXR activity. T0901317 directly binds retinoic acid receptor-related orphan receptors RORalpha and RORgamma with high affinity (K(i) = 132 and 51nM, respectively) resulting in the modulation of the receptor's ability to interact with transcriptional cofactor proteins. T0901317 acts as an antiandrogen for AR in prostate cancer cells. T0901317 shows anti-atherosclerosis, antidiabetic, insulin sensitizing, anticancer, anti-proliferative, metabolism modulating and neuroprotective properties. Exhibits inverse agonist activity at human constitutive androstane receptor (CAR), a member of the nuclear receptor superfamily and key regulator of xenobiotic and endobiotic metabolism.

+4°C

Ambient

481.3

solid

瑞士

>97%

293754-55-9

C17H12F9NO3S