| Bioactivity | 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]. |
| Invitro | Reverse transcriptase-IN-4 (compound F10) (0-10 μM) 对所 CYP 酶表现出非常弱的抑制作用。其中,对 CYP1A2、CYP2D6、CYP3A4T、CYP3A4M 的抑制活性超过 50 μM。对 CYP2C9 和 CYP2C19 无明显抑制作用,IC50 值分别为 35.8 μM 和 27.1 μM[1]。 |
| In Vivo | Reverse transcriptase-IN-4 (compound F10) (1.0 g/kg, p.o) 在小鼠中耐受性良好,没有急性毒性,具有良好的体内安全性[1]。 |
| Name | Reverse transcriptase-IN-4 |
| Formula | C17H21N5OS |
| Molar Mass | 343.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |