1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV Protease
  3. TMC310911

TMC310911 

Cat. No.: HY-107123
Handling Instructions

TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity.

For research use only. We do not sell to patients.

TMC310911 Chemical Structure

TMC310911 Chemical Structure

CAS No. : 1000287-05-7

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Description

TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity[1][2].

IC50 & Target

EC50: 2.2-14.2 nM (Wild-type HIV-1)[1]

In Vitro

For a panel of 2,011 recombinant isolates with decreased susceptibility to at least one of the currently approved protease inhibitors (PIs), the FC in TMC310911 EC50 is ≤4 for 82% of isolates and ≤10 for 96% of isolates. The fold change (FC) in TMC310911 EC50 is ≤4 and ≤10 for 72% and 94% of isolates with decreased susceptibility to Darunavir, respectively. In vitro resistance selection (IVRS) performed with r13025, a multiple-PI-resistant recombinant isolate, and TMC310911 selected for mutations L10F, I47V, and L90M (FC in TMC310911 EC50 = 16)[1].
The TMC310911 EC50 values against HIV-1/LAI and HIV-2/ROD in MT4 cells with EC50 values of 14.2 nM and 2 nM, respectively, and HIV-1/LAI and HIV-1/SF2 in PBMCs with EC50 values of 2.2 nM and 2.3 nM, respectively, and HIV-1/BaL in M/M cells with an EC50 value of 13.9 nM. And the corresponding EC90 values ranged from 5.0 to 94.7 nM. The TMC310911 CC50 for MT4 cells is 9.9 μM[1].

Molecular Weight

755.99

Formula

C₃₈H₅₃N₅O₇S₂

CAS No.

1000287-05-7

SMILES

O=C(O[[email protected]@H]1[[email protected]@]2([H])[[email protected]@](OCC2)([H])OC1)N[[email protected]@H](CC3=CC=CC=C3)[[email protected]](O)CN(S(=O)(C4=CC=C5N=C(NC6CCN(C7CCCC7)CC6)SC5=C4)=O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TMC310911TMC 310911TMC-310911HIV ProteaseDarunavirHIV-1antiviralrecombinantmultiple-PI-resistantbroadsusceptibilitygeneticbarrierInhibitorinhibitorinhibit

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