HIV-1 integrase inhibitor 10
HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1).
For research use only. We do not sell to patients.
- Formula: C40H45N7O4
- Molecular Weight:687.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
EC50 for NLRepRluc virus: 3.9 nM (T/T); 4.5 nM (N/A); 5.2 nM (A/A)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT2 | CC50 |
>=3 μM
Compound: 11
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Cytotoxicity against human MT2 cells infected with HIV1 NLRep-Rluc harbouring polymorphic 124T/125T integrase
Cytotoxicity against human MT2 cells infected with HIV1 NLRep-Rluc harbouring polymorphic 124T/125T integrase
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[PMID: 35605346] |
HIV-1 integrase inhibitor 10 (compound 11) has excellent antiviral potency for viruses containing the T/T, N/A and A/A polymorphs with EC50 values of 3.9 nM, 4.5 nM and 5.2 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:1 mg/kg, 5 mg/kg
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Administration:1 mg/kg, iv. and 5 mg/kg, po., as solutions in 90:10 PEG-400:EtOH for IV dosing and 90:5:5 PEG-400:EtOH:TPGS for PO dosing.
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Result:
Compound Rat Cl (mL/min/kg) Rat AUC0-∞ (nMhr) Rat %F PAMPA permeability (nM/sec) at pH 5.5/7.4 HIV-1 integrase inhibitor 10 (Compound 11) 2.8 36,305 83% 1009/752
Chemical Information
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Molecular Weight 687.83
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Formula C40H45N7O4
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SMILES
CC1=NN2C(C(C3=CC=C4CN(CCC4=C3)C5=NC=NC6=C5OC7=C6C=CC=C7)=C(C([C@@H](C(O)=O)OC(C)(C)C)=C2C)N8CCC(C)(CC8)C)=N1
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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)