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

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.

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HIV-1 inhibitor-8 Chemical Structure

HIV-1 inhibitor-8 Chemical Structure

CAS No. : 2826996-78-3

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Based on 1 publication(s) in Google Scholar

HIV-1 inhibitor-8 Related Antibodies

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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.

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

HIV-1 inhibitor-8 Related Antibodies
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].

MedChemExpress (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
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

N#CC1=CC=C(NC2=NC(OC3=C(C)C=C(/C=C/C#N)C=C3C)=C(CSCC4)C4=N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (113.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2752 mL 11.3758 mL 22.7516 mL
5 mM 0.4550 mL 2.2752 mL 4.5503 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2752 mL 11.3758 mL 22.7516 mL 56.8789 mL
5 mM 0.4550 mL 2.2752 mL 4.5503 mL 11.3758 mL
10 mM 0.2275 mL 1.1376 mL 2.2752 mL 5.6879 mL
15 mM 0.1517 mL 0.7584 mL 1.5168 mL 3.7919 mL
20 mM 0.1138 mL 0.5688 mL 1.1376 mL 2.8439 mL
25 mM 0.0910 mL 0.4550 mL 0.9101 mL 2.2752 mL
30 mM 0.0758 mL 0.3792 mL 0.7584 mL 1.8960 mL
40 mM 0.0569 mL 0.2844 mL 0.5688 mL 1.4220 mL
50 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1376 mL
60 mM 0.0379 mL 0.1896 mL 0.3792 mL 0.9480 mL
80 mM 0.0284 mL 0.1422 mL 0.2844 mL 0.7110 mL
100 mM 0.0228 mL 0.1138 mL 0.2275 mL 0.5688 mL
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HIV-1 inhibitor-8 Related Classifications

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-82826996-78-3HIVHuman immunodeficiency virusorallyactivelow-toxicitypotentnon-nucleosidereversetranscriptaseInhibitorinhibitorinhibit

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