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1610763-24-0

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1610763-24-0 Usage

Check Digit Verification of cas no

The CAS Registry Mumber 1610763-24-0 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,6,1,0,7,6 and 3 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1610763-24:
(9*1)+(8*6)+(7*1)+(6*0)+(5*7)+(4*6)+(3*3)+(2*2)+(1*4)=140
140 % 10 = 0
So 1610763-24-0 is a valid CAS Registry Number.

1610763-24-0Relevant articles and documents

Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane x receptor antagonists

Hodnik, ?iga,Peterlin Ma?i?, Lucija,Toma?i?, Tihomir,Smodi?, Domen,D'Amore, Claudio,Fiorucci, Stefano,Kikelj, Danijel

, p. 4819 - 4833 (2014/07/07)

Pregnane X receptor (PXR), a member of the NR1I nuclear receptor family, acts as a xenobiotic sensor and a paramount transcriptional regulator of drug-metabolizing enzymes and transporters. The overexpression of PXR in various cancer cells indicates the importance of PXR as a drug target for countering multidrug resistance in anticancer treatments. We describe the discovery of novel bazedoxifene-scaffold-based PXR antagonists inspired by the marine sulfated steroids solomonsterol A and B as natural leads. A luciferase reporter assay on a PXR-transfected HepG2 cell line identified compounds 19-24 as promising PXR antagonists. Further structure-activity relationship studies of the most active PXR antagonist from the series (compound 20, IC50 = 11 μM) revealed the importance of hydroxyl groups as hydrogen-bond donors for PXR antagonistic activity. PXR antagonists 20 and 24 (IC50 = 14 μM), in addition to the downregulation of PXR expression, exhibited inhibition of PXR-induced CYP3A4 expression, which illustrates their potential to suppress PXR-regulated phase-I drug metabolism.

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