产品
编 号：F756202
分子式：C25H21N5OS
分子量：439.53
分子式：C25H21N5OS
分子量：439.53
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
询价
询价
10mg
询价
询价
25mg
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询价
结构图
CAS No: 2826996-78-3
产品详情
生物活性：
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV?1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV?1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.
体内研究：
HIV-1 inhibitor-8 (2 mg/kg; i.v.) shows a favorable mean CL, volume of distribution and a long terminal half-life.HIV-1 inhibitor-8 (20 mg/kg; p.o.) absorption reaches maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time is 2.90 hours.Animal Model:Sprague-Dawley (SD) rat
Dosage:2 mg/kg
Administration:I.v.
Result:Showed a favorable mean CL, volume of distribution and a long terminal half-life.
Animal Model:Sprague-Dawley (SD) rat
Dosage:20 mg/kg
Administration:P.o.
Result:Absorption reached maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time was 2.90 hours.
体外研究：
HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV-1 strains and improves resistance profiles (RF = 0.5~5.6). HIV-1 inhibitor-8 exhibits reduces cytotoxicity (CC50=284 μM) and higher SI values (SI = 5210~63992). HIV-1 inhibitor-8 displays better solubility (sol. =12.8 μg/mL) and no significant inhibition of the main CYP enzymes. HIV-1 inhibitor-8 displays an extremely low hERG inhibition with an IC50 value of 19.84 μM in CHO-hERG cells.
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV?1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV?1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.
体内研究：
HIV-1 inhibitor-8 (2 mg/kg; i.v.) shows a favorable mean CL, volume of distribution and a long terminal half-life.HIV-1 inhibitor-8 (20 mg/kg; p.o.) absorption reaches maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time is 2.90 hours.Animal Model:Sprague-Dawley (SD) rat
Dosage:2 mg/kg
Administration:I.v.
Result:Showed a favorable mean CL, volume of distribution and a long terminal half-life.
Animal Model:Sprague-Dawley (SD) rat
Dosage:20 mg/kg
Administration:P.o.
Result:Absorption reached maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time was 2.90 hours.
体外研究：
HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV-1 strains and improves resistance profiles (RF = 0.5~5.6). HIV-1 inhibitor-8 exhibits reduces cytotoxicity (CC50=284 μM) and higher SI values (SI = 5210~63992). HIV-1 inhibitor-8 displays better solubility (sol. =12.8 μg/mL) and no significant inhibition of the main CYP enzymes. HIV-1 inhibitor-8 displays an extremely low hERG inhibition with an IC50 value of 19.84 μM in CHO-hERG cells.
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