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编 号：F762836
分子式：C24H18F3N5O3
分子量：481.43
分子式：C24H18F3N5O3
分子量：481.43
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CAS No: 3033486-43-7
产品详情
生物活性：
ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS.
体内研究：
Zlm-66 (1-5 mg/kg; i.v. and p.o. once) shows good druggability and have a good effect in vivo after oral administration.1.19Pharmacokinetic Parameters of ZLM-66 in rat.RatIV 1 mg/kg RatPO 5 mg/kg
T1/2 (h)1.90±0.288.45±4.88
Tmax (h)0.08±0.006.67±1.15
Cmax (ng/mL)468.67±63.09583.33±290.11
AUC0-t (h*ng/ml)891.94±79.304983.22±3220.11
AUC0-∞ (h*ng/ml)940.41±105.006594.05±1547.74
CL (ml/h/kg)1072.31±120.40791.14±210.66/tr>MRT0-t (h)2.03±0.26.79±1.90/tr>MRT0-∞ (h)2.48±0.3513.92±6.44
F (%)140.24
Animal Model:Six- to 8-week-old male Sprague-Dawley rats (180?230 g)
Dosage:1, 5 mg/kg
Administration:Intravenous injection, oral gavage;1-5 mg/kg; once
Result:Possed a better in vivo effect of oral administration with half-life, plasma clearance and oral bioavailability of 8.45 h, 791.14 ml/h/kg and 140.24% respectively.
体外研究：
ZLM-66 (0.0016-125 μg/ml, 5 d) inhibits HIV-1 and HIV-1 mutant strains in MT-4 cells.
ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS.
体内研究：
Zlm-66 (1-5 mg/kg; i.v. and p.o. once) shows good druggability and have a good effect in vivo after oral administration.1.19Pharmacokinetic Parameters of ZLM-66 in rat.RatIV 1 mg/kg RatPO 5 mg/kg
T1/2 (h)1.90±0.288.45±4.88
Tmax (h)0.08±0.006.67±1.15
Cmax (ng/mL)468.67±63.09583.33±290.11
AUC0-t (h*ng/ml)891.94±79.304983.22±3220.11
AUC0-∞ (h*ng/ml)940.41±105.006594.05±1547.74
CL (ml/h/kg)1072.31±120.40791.14±210.66/tr>MRT0-t (h)2.03±0.26.79±1.90/tr>MRT0-∞ (h)2.48±0.3513.92±6.44
F (%)140.24
Animal Model:Six- to 8-week-old male Sprague-Dawley rats (180?230 g)
Dosage:1, 5 mg/kg
Administration:Intravenous injection, oral gavage;1-5 mg/kg; once
Result:Possed a better in vivo effect of oral administration with half-life, plasma clearance and oral bioavailability of 8.45 h, 791.14 ml/h/kg and 140.24% respectively.
体外研究：
ZLM-66 (0.0016-125 μg/ml, 5 d) inhibits HIV-1 and HIV-1 mutant strains in MT-4 cells.
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