Bioactivity | HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056)[1]. |
In Vivo | HIV-1 inhibitor-51 (化合物 36a·HCl; 2 mg/kg; 静脉给药) 的 T1/2 为 1.43 小时,CL 为 103 L/h·kg,Cmax 为 484 ng/mL[1]。 HIV-1 inhibitor-51 (10 mg/kg; 口服) 的 T1/2 为 5.12 小时,Cmax 为 37.5 ng/mL[1]。 Animal Model: |
Name | HIV-1 inhibitor-51 |
CAS | 2834087-82-8 |
Formula | C24H19ClFN5O2 |
Molar Mass | 463.89 |
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]. Yanying Sun, et al. Lead Optimization and Avoidance of Metabolic-perturbing Motif Developing Novel Diarylpyrimidines as Potent HIV-1 NNRTIs. J Med Chem. 2022 Dec 8;65(23):15608-15626. |