HIV-1 inhibitor-52

Names

[ CAS No. ]:
1818868-23-3

[ Name ]:
HIV-1 inhibitor-52

Biological Activity

[Description]:

HIV-1 inhibitor-52 is a potent broad-spectrum HIV-1 activity inhibitor with EC50s of 1.6 nM-6.4 nM for WT HIV-1, HIV-1 V370A, HIV-1 ΔV370, HIV-1 V362I/V370A, HIV-1 T332S/V362I/prR41G, HIV-1 A326T/V362I/V370A, HIV-1 R361K/V362I/L363M[1].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HIV
Research Areas >> Infection

[Target]

HIV-1 (WT):1.6 nM (EC50)

HIV-1 V370A:3.0 nM (EC50)

HIV-1 ΔV370:5.1 nM (EC50)

HIV-1 V362I/V370A:2.0 nM (EC50)

HIV-1 T332S/V362I/prR41G:6.4 nM (EC50)

HIV-1 A326T/V362I/V370A:4.3 nM (EC50)

HIV-1 R361K/V362I/L363M:4.5 nM (EC50)


[In Vivo]

HIV-1 inhibitor-52 (化合物 26; 1 mg/kg; 静脉给药) 在大鼠的 T1/2 为 4.2 小时，CL 为 3.5 mL/min·kg，Vss 为 0.8 L/kg[1]。 HIV-1 inhibitor-52 (5 mg/kg; 灌胃) 对大鼠的 Cmax 为 0.83 μM，AUC 为 8.11 μM·h[1]。 Animal Model: Male sprague-dawley rats[1] Dosage: 1 mg/kg Administration: IV Result: Had a T1/2 of 4.2 hours, a CL of 3.5 mL/min•kg, and a Vss of 0.8 L/kg for rats.

[References]

[1]. Richard A Hartz, et al. Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad Spectrum Activity. J Med Chem. 2022 Dec 8;65(23):15935-15966.  

Chemical & Physical Properties

[ Molecular Formula ]:
C46H72FNO5S

[ Molecular Weight ]:
770.13

Related Compounds