((plusmn))-BI-D


CAS No. : 1416258-16-6

((plusmn))-BI-D,1416258-16-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I013834
Molecular Formula:C₂₅H₂₇NO₄
Molecular Weight:405.49
Target: HIV HIV Integrase
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Cat No:I013834
Cas No:1416258-16-6
Product-Name:((plusmn))-BI-D
IUPAC Name:2-[4-(3,4-dihydro-2H-chromen-6-yl)-2-methylquinolin-3-yl]-2-[(2-methylpropan-2-yl)oxy]acetic acid
InChI:InChI=1S/C25H27NO4/c1-15-21(23(24(27)28)30-25(2,3)4)22(18-9-5-6-10-19(18)26-15)17-11-12-20-16(14-17)8-7-13-29-20/h5-6,9-12,14,23H,7-8,13H2,1-4H3,(H,27,28)
InChIKey:ZFERZAMPQIXCPM-UHFFFAOYSA-N
SMILES:CC1=NC2=CC=CC=C2C(=C1C(C(=O)O)OC(C)(C)C)C3=CC4=C(C=C3)OCCC4
(±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site. IC50 value: 2.4–2.9 μM(HIV-Luc infection of WT and Hdgfrp2 KO cells) [1] Target: integrase inhibitor in vitro: Approximately 2.4–2.9 μM of BI-D was required to inhibit 50% of HIV-Luc infection of WT and Hdgfrp2 KO cells, while the IC50 decreased dramatically, to 160–200 nM, in Psip1 and double-KO cells [1].
[1]. Wang H, et al. HRP2 determines the efficiency and specificity of HIV-1 integration in LEDGF/p75 knockout cells but does not contribute to the antiviral activity of a potent LEDGF/p75-binding site integrase inhibitor. Nucleic Acids Res. 2012 Dec;40(22):115
[2]. Fader LD, et al. Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV. ACS Med Chem Lett. 2014 Apr 16;5(6):711-6.
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