HIV-1 inhibitor-52

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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.

For research use only. We do not sell to patients.

HIV-1 inhibitor-52 Chemical Structure

CAS No. : 1818868-23-3

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

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 (compound 26; 1 mg/kg; IV) has a T_1/2 of 4.2 hours, a CL of 3.5 mL/min·kg, and a V_ss of 0.8 L/kg for rats^[1].
HIV-1 inhibitor-52 (5 mg/kg; po) has a C_max of 0.83 μM and an AUC of 8.11 μM·h for rats^[1].

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

Animal Model:	Male sprague-dawley rats^[1]
Dosage:	1 mg/kg
Administration:	IV
Result:	Had a T_1/2 of 4.2 hours, a CL of 3.5 mL/min•kg, and a V_ss of 0.8 L/kg for rats.

Molecular Weight

770.13

Formula

C₄₆H₇₂FNO₅S

CAS No.

1818868-23-3

SMILES

O[C@]1(CC[C@@H](CC1)S(C)(=O)=O)CCN[C@]23[C@@]([C@@H](CC3)C(C)=C)([H])[C@]4([H])[C@@](CC2)([C@]5([C@]([C@@]6([C@@](C(C)(C(C7=CC[C@@](C(O)=O)(CF)CC7)=CC6)C)([H])CC5)C)([H])CC4)C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]