2. Anti-infection
  3. Reverse Transcriptase HIV
  4. NNRT-IN-13

NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly inhibiting HIV-1 reverse transcriptase (IC₅₀ = 0.25 μM). NNRT-IN-13 exhibits excellent antiviral activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants. NNRT-IN-13 exhibits favorable in vivo metabolic and safety profiles. NNRT-IN-13 can be used for human immunodeficiency virus (HIV) research.

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NNRT-IN-13

NNRT-IN-13 Chemical Structure

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NNRT-IN-13 Related Antibodies

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Description

NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly inhibiting HIV-1 reverse transcriptase (IC₅₀ = 0.25 μM). NNRT-IN-13 exhibits excellent antiviral activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants. NNRT-IN-13 exhibits favorable in vivo metabolic and safety profiles. NNRT-IN-13 can be used for human immunodeficiency virus (HIV) research[1].

In Vitro

NNRT-IN-13 (compound 15k) exhibits excellent activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants, including L100I (0.0053 μM), K103N (0.0034 μM), Y181C (0.010 μM), Y188L (0.026 μM), E138 K (0.015 μM), F227L/V106A (0.033μM), and K103N/Y181C (0.029 μM), while displaying low cytotoxicity in MT-4 cells (CC50 = 26.64 μM)[1].
NNRT-IN-13 binds HIV-1 reverse transcriptase in a unique "Y-shaped" mode, forming novel hydrogen bonds with the p51-p66 interface residues E138 and K101[1].
NNRT-IN-13 exhibits no inhibition toward CYP1A2, CYP2C9, CYP2C19, and CYP2D6, with IC50 values exceeding 50 μM, and shows weak inhibition of CYP3A4M (IC50 = 13.6 μM)[1].

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

NNRT-IN-13 Related Antibodies
In Vivo

NNRT-IN-13 (50 and 2000 mg/kg, i.p., single dose or every other day for 14 days) exhibits no toxicity and induces no organ damage in Kunming mice[1].

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

Animal Model: Kunming mice[1]
Dosage: 2000 mg/kg
Administration: i.p., single dose
Result: Showed no mortality or adverse toxicity signs, including anorexia, lethargy, alopecia, or dyspnea.
Exhibited steady weight gain over the seven-day observation period, with no significant differences compared to control.
Animal Model: Kunming mice[1]
Dosage: 50 mg/kg
Administration: i.p., every other day for 14 days
Result: Showed no apparent toxicity signs or behavioral abnormalities (such as lethargy, clonic convulsions, anorexia, and ruffled fur.
Gained normal body weight and were equivalent to those of the control group.
Exhibited no visible pathological changes or lesions were detected in the heart, liver, spleen, lungs, or kidneys.
Molecular Weight

614.72

Formula

C31H34N8O4S
SMILES

O=S(C1=CC=C(CN2CCC(NC3=NC(OC4=C(C=C(C=C4C)/C=C/C#N)C)=CC(NCC5=COC=N5)=N3)CC2)C=C1)(N)=O
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References
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NNRT-IN-13 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:

NNRT-IN-13Reverse TranscriptaseHIVHuman immunodeficiency virusNNRTHIV-1MT-4 cellsInhibitorinhibitorinhibit

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