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

Darunavir (Synonyms: TMC114; UIC-94017)

Cat. No.: HY-17040 Purity: 99.90%
Handling Instructions

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity.

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

Darunavir Chemical Structure

Darunavir Chemical Structure

CAS No. : 206361-99-1

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 210 In-stock
Estimated Time of Arrival: December 31
5 mg USD 174 In-stock
Estimated Time of Arrival: December 31
10 mg USD 318 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1176 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

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Description

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity[1][2].

In Vitro

Darunavir (TMC114, 1a) has a stability comparable to other protease inhibitors[1].
Darunavir (TMC114, UIC-94017) blocks the infectivity and replication of each of HIV-1NL4-3 variants exposed to and selected for resistance to Ro 31-8959, MK-639, AG1341, or ABT 538 at concentrations up to 5 μM (IC50s, 0.003 to 0.029 μM), although it was less active against HIV-1NL4-3 variants selected for resistance to VX-478 (IC50, 0.22 μM)[2].

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

Clinical Trial
Molecular Weight

547.66

Formula

C₂₇H₃₇N₃O₇S

CAS No.

206361-99-1

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=C(N)C=C4)=O)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (182.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8260 mL 9.1298 mL 18.2595 mL
5 mM 0.3652 mL 1.8260 mL 3.6519 mL
10 mM 0.1826 mL 0.9130 mL 1.8260 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DarunavirTMC114 UIC-94017TMC 114TMC-114UIC94017UIC 94017UIC-94017HIVHIV ProteaseHuman immunodeficiency virusMinimalcytotoxicityAIDHIV,Inhibitorinhibitorinhibit

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Darunavir
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