Reverse transcriptase-IN-1

Research use only, not for human use.

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM. (In Vitro):Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively.(In Vivo):The PK study and safety assessment of Reverse transcriptase-IN-1 shows that it is absorbed with mean residence times (MRTs) of 11.8 hours (5 mg/kg, p.o.) and 11.4 hours (1 mg/kg, i.v.) at these two doses. The Cmax of Reverse transcriptase-IN-1 is 39.9 ng/mL at a dose of 5 mg/kg. The oral bioavailability of Reverse transcriptase-IN-1 is significantly improved to 16.5% at a dose of 5 mg/kg in rats. The intrinsic rat microsome clearance of Reverse transcriptase-IN-1 is 33.2 μL/min/mg proteins.

——

Microbiology/Virology

HIV

——

——

——

2380001-43-2

447.5

C25H17N7O2

>98% (HPLC)

——

Cc1cc(\C=C\C#N)cc(c1Nc1nc(Nc2ccc(cc2)C#N)nc2ccccc12)[N+]([O-])=O

——

(-20℃)

With Ice Pack

≥ 2 years