HIV-1 inhibitor-49
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model.
For research use only. We do not sell to patients.
- CAS No.: 3038135-11-1
- Formula: C21H18F2N2O3S
- Molecular Weight:416.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HIV-1 (WT) 17 nM (EC50) |
HIV-1 (L100I) 0.38 μM (EC50) |
HIV-1 (K103N) 2.64 μM (EC50) |
HIV-1 (Y181C) 1.85 μM (EC50) |
HIV-1 (E138K) 0.09 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
39.21 μM
Compound: 9h
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Cytotoxicity against human MT4 cells assessed as reduction in cell viability
Cytotoxicity against human MT4 cells assessed as reduction in cell viability
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[PMID: 36442370] |
HIV-1 inhibitor-49 (compound 9h) (EC50=17 nM-39.21 μM) inhibits WT HIV-1 with much higher selectivity index over other HIV-1 mutant (L100I, K103N, Y181C, and E138K)[1].
HIV-1 inhibitor-49 (0-50 μM) shows little CYP enzyme, hERG inhibition in CHO-hERG cells, with IC50s of 27.6 μM (CYP2C9), 30.3 μM (CYP2C19), and >50 μM (others)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HIV-1 inhibitor-49 (10 mg/kg; p.o.; single dose) shows excellent oral bioavailability in rats[1].
Rat PK profile[1]
| Route | Dose (mg/kg) | AUC0-t (ng·h/mL) | AUC0-∞ (ng·h/mL) | T1/2 (h) | Tmax (h) | Vz (mL/kg) | Cl (mL/h/kg) | Cmax (ng/mL) | F (%) |
| i.v. | 1.0 | 1102 | 1100 | 0.514 | 0.083 | 698 | 936 | 2033 | |
| p.o. | 10 | 9557 | 8663 | 2.51 | 0.583 | 3523 | 86.72% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3038135-11-1
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Molecular Weight 416.44
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Formula C21H18F2N2O3S
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SMILES
O=C1NC(N(C(SC2=CC(F)=CC=C2F)=C1C3CC3)COCC4=CC=CC=C4)=O
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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)
HIV-1 inhibitor-49 Related Classifications
HY-151933 Related Classifications
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