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

Darunavir Ethanolate (Synonyms: TMC114 (Ethanolate))

Cat. No.: HY-17041 Purity: 99.73%
Handling Instructions

Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.

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

Darunavir Ethanolate Chemical Structure

Darunavir Ethanolate Chemical Structure

CAS No. : 635728-49-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 94 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.

IC50 & Target

Ki: 1 nM (WT HIV-1 protease)[1]

In Vitro

Darunavir is a broad-spectrum potent inhibitor active against HIV-1 clinical isolates with minimal cytotoxicity. Darunavir forms hydrogen bonds with the conserved main-chain atoms of Asp29 and Asp30 of the protease. These interactions are proposed to be critical for the potency of this compound against HIV isolates that are resistant to multiple protease inhibitors[1]. In an in vitro study in MT-2 cells, the potency of darunavir is greater than that of saquinavir, amprenavir, nelfinavir, indinavir, lopinavir and ritonavir. Darunavir is primarily metabolized by the hepatic cytochrome P450 (CYP) enzymes, primarily CYP3A. The ‘boosting’ dose of ritonavir acts an an inhibitor of CYP3A, thereby increasing darunavir bioavailability[2].

In Vivo

Darunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It needs to be combined with ritonavir, which increases the bioavailability to 82%[3].

Clinical Trial
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 : ≥ 50 mg/mL (84.21 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6843 mL 8.4213 mL 16.8427 mL
5 mM 0.3369 mL 1.6843 mL 3.3685 mL
10 mM 0.1684 mL 0.8421 mL 1.6843 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

593.73

Formula

C₂₉H₄₃N₃O₈S

CAS No.

635728-49-3

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.CCO

Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
Darunavir Ethanolate
Cat. No.:
HY-17041
Quantity:

Darunavir Ethanolate

Cat. No.: HY-17041