Reverse transcriptase-IN-4 

Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC₅₀ value of 0.053 μM for wild-type HIV-1 and an EC₅₀ value of 0.26 μM for HIV-1 mutant E138K^[1]. Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

Reverse transcriptase-IN-4 (compound F10) (0-10 μM) shows very weak inhibitory effects on all CYP enzymes, and the inhibitory activities of CYP1A2, CYP2D6, CYP3A4T and CYP3A4M exceeds 50 μM. No significant inhibition is observed for CYP2C9 and CYP2C19, with IC₅₀ values of 35.8 μM and 27.1 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reverse transcriptase-IN-4 (compound F10) (1.0 g/kg, p.o) is well tolerated in mice, has no acute toxicity and has a good in vivo safety profile^[1]。

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

343.45

C₁₇H₂₁N₅OS

CC1=CC(C)=CC(C(C2=C(C(NC(SC(C)C)=N2)=O)C)N=[N+]=[N-])=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Xu Ling, et al. Development of novel S-N3-DABO derivatives as potent non-nucleoside reverse transcriptase inhibitors with improved potency and selectivity. Eur J Med Chem. 2022 Dec 23;247:115042.  [Content Brief]