HIV-1 inhibitor-50
HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC50=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains.
For research use only. We do not sell to patients.
- CAS No.: 2834087-69-1
- Formula: C24H18FN5O2
- Molecular Weight:427.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HIV-1 (WT) 3.04 nM (EC50) |
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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
45.6 μM
Compound: 36a
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
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[PMID: 36411036] |
HIV-1 inhibitor-50 (compound 36a) protects MT-4 cells from HIV-1 IIIB and RES056 with EC50s of 2.22 nM and 53.3 nM, respectively[1].
HIV-1 inhibitor-50 inhibits MT-4 cells viability with an CC50 value of 45.6 μM[1].
HIV-1 inhibitor-50 (hydrochloride; ) shows a lower intrinsic clearance rates in microsomes (CL=87.6 μL/min/mg) and liver (CL=16.6 μL/min/mg), and leads to a higher metabolic stability (T1/2=11.3 min)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MT-4 cells
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Concentration:
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Incubation Time:
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Result:Inhibited HIV-1 infection in MT-4 cells with EC50 values of 3.04 nM (L100I), 2.87 nM (K103N), 10.2 nM (Y181C), 13.2 nM (Y188L), 9.77 nM (E138K), 19.8 nM (F227L+V106A), respectively.
HIV-1 inhibitor-50 (hydrochloride; 2000 mg/kg; p.o.; single dose) doesn’t result any abnormal behaviors or significant changes in body weight compared with the control in 7 days, indicating no acute toxicity[1].
Pharmacokinetic Analysis[1]
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (h·ng/mL) | AUC0-∞ (h·ng/mL) | CL (L/h/kg) | F (%) |
| i.v. | 2 | 1.43 | 0 | 484 | 250 | 255 | 103 | / |
| p.o. | 10 | 5.12 | 0.25 | 37.5 | 107 | 154 | / | 12.1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2834087-69-1
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Molecular Weight 427.43
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Formula C24H18FN5O2
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SMILES
CC1=C(OC2=C3COCC3=NC(NC4=CC(F)=C(C=C4)C#N)=N2)C(C)=CC(/C=C/C#N)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)