[CAS NO. 2834087-82-8]  HIV-1 inhibitor-51

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PRODUCTS SPECIFICATIONS [2834087-82-8]

Catalog
HY-152161
Brand
MCE
CAS
2834087-82-8

DESCRIPTION [2834087-82-8]

Overview

MDL-
Molecular Weight463.89
Molecular FormulaC24H19ClFN5O2
SMILESFC(C=C1NC2=NC(OC3=C(C=C(C=C3C)/C=C/C#N)C)=C4C(COC4)=N2)=C(C=C1)C#N.Cl

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

Summary

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 ( K D =2.50 μM) and inhibitory activity ( IC 50 =0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC 50 s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) [1] .


IC50 & Target

HIV-1 (WT)

0.03 μM (IC 50 )

HIV-1 (WT)

2.5 μM (Kd)

HIV-1 (L100I)

3.04 nM (EC 50 )

HIV-1 (K103N)

2.87 nM (EC 50 )

HIV-1 (Y181C)

10.2 nM (EC 50 )

HIV-1 (Y188L)

13.2 nM (EC 50 )

HIV-1 (E138K)

9.77 nM (EC 50 )

HIV-1 (F227L+V106A)

19.8 nM (EC 50 )

HIV-1 (RES056)

53.3 nM (EC 50 )


In Vivo

HIV-1 inhibitor-51 (compound 36a·HCl; 2 mg/kg; iv) has a T 1/2 of 1.43 hours, a CL of 103 L/h·kg, and C max of 484 ng/mL [1] .
HIV-1 inhibitor-51 (10 mg/kg; orally) has a T 1/2 of 5.12 hours, and C max of 37.5 ng/mL [1] .

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

Animal Model: ICR mice [1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T 1/2 of 5.12 hours, and C max of 37.5 ng/mL.

Shipping

Room temperature in continental US; may vary elsewhere.


Storage

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