1. Anti-infection
  2. HIV
  3. HIV-1 inhibitor-8

HIV-1 inhibitor-8 

Cat. No.: HY-132291
Handling Instructions

HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.

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

HIV-1 inhibitor-8 Chemical Structure

HIV-1 inhibitor-8 Chemical Structure

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Description

HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM[1].

IC50 & Target[1]

HIV-1 (WT)

0.081 μM (IC50)

In Vitro

HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV-1 strains and improves resistance profiles (RF = 0.5~5.6). HIV-1 inhibitor-8 exhibits reduces cytotoxicity (CC50=284 μM) and higher SI values (SI = 5210~63992). HIV-1 inhibitor-8 displays better solubility (sol. =12.8 μg/mL) and no significant inhibition of the main CYP enzymes. HIV-1 inhibitor-8 displays an extremely low hERG inhibition with an IC50 value of 19.84 μM in CHO-hERG cells.

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

In Vivo

HIV-1 inhibitor-8 (2 mg/kg; i.v.) shows a favorable mean CL, volume of distribution and a long terminal half-life[1].
HIV-1 inhibitor-8 (20 mg/kg; p.o.) absorption reaches maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time is 2.90 hours[1].

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

Animal Model: Sprague-Dawley (SD) rat[1]
Dosage: 2 mg/kg
Administration: I.v.
Result: Showed a favorable mean CL, volume of distribution and a long terminal half-life.
Animal Model: Sprague-Dawley (SD) rat[1]
Dosage: 20 mg/kg
Administration: P.o.
Result: Absorption reached maximum at 0.25 hours with a plasma concentration value of 16.6 ng/mL and the mean residence time was 2.90 hours.
Molecular Weight

439.53

Formula

C₂₅H₂₁N₅OS

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Product Name:
HIV-1 inhibitor-8
Cat. No.:
HY-132291
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