2. Anti-infection
  3. HIV Reverse Transcriptase
  4. HIV-1 inhibitor-51

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).

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HIV-1 inhibitor-51 Chemical Structure

HIV-1 inhibitor-51 Chemical Structure

CAS No. : 2834087-82-8

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HIV-1 inhibitor-51 Related Antibodies

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Description

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].

IC50 & Target[1]

HIV-1 (WT)

0.03 μM (IC50)

HIV-1 (WT)

2.5 μM (Kd)

HIV-1 (L100I)

3.04 nM (EC50)

HIV-1 (K103N)

2.87 nM (EC50)

HIV-1 (Y181C)

10.2 nM (EC50)

HIV-1 (Y188L)

13.2 nM (EC50)

HIV-1 (E138K)

9.77 nM (EC50)

HIV-1 (F227L+V106A)

19.8 nM (EC50)

HIV-1 (RES056)

53.3 nM (EC50)

In Vivo

HIV-1 inhibitor-51 (compound 36a·HCl; 2 mg/kg; iv) has a T1/2 of 1.43 hours, a CL of 103 L/h·kg, and Cmax of 484 ng/mL[1].
HIV-1 inhibitor-51 (10 mg/kg; orally) has a T1/2 of 5.12 hours, and Cmax of 37.5 ng/mL[1].

MedChemExpress (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 T1/2 of 5.12 hours, and Cmax of 37.5 ng/mL.
Molecular Weight

463.89

Formula

C24H19ClFN5O2
CAS No.
SMILES

FC(C=C1NC2=NC(OC3=C(C=C(C=C3C)/C=C/C#N)C)=C4C(COC4)=N2)=C(C=C1)C#N.Cl
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
References
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HIV-1 inhibitor-51 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HIV-1 inhibitor-512834087-82-8HIVReverse TranscriptaseHuman immunodeficiency virusnon-nucleoside reverse transcriptaseNNRTIantiviral activity,WT HIV-1 (IIIB)L100IK103NY181CY188LE138KF227LV106ARES056Inhibitorinhibitorinhibit

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