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

Darunavir  (Synonyms: TMC114; UIC-94017)

Cat. No.: HY-17040 Purity: 99.84%
COA Handling Instructions

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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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 48 In-stock
Solution
10 mM * 1 mL in DMSO USD 48 In-stock
Solid
5 mg USD 40 In-stock
10 mg USD 60 In-stock
25 mg USD 90 In-stock
50 mg USD 140 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 10 publication(s) in Google Scholar

Other Forms of Darunavir:

Darunavir Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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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].

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

Darunavir Related Antibodies
Clinical Trial
Molecular Weight

547.66

Formula

C27H37N3O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@H]1[C@@]2([H])[C@@](OCC2)([H])OC1)N[C@@H](CC3=CC=CC=C3)[C@H](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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (182.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

COA (261 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8260 mL 9.1298 mL 18.2595 mL 45.6488 mL
5 mM 0.3652 mL 1.8260 mL 3.6519 mL 9.1298 mL
10 mM 0.1826 mL 0.9130 mL 1.8260 mL 4.5649 mL
15 mM 0.1217 mL 0.6087 mL 1.2173 mL 3.0433 mL
20 mM 0.0913 mL 0.4565 mL 0.9130 mL 2.2824 mL
25 mM 0.0730 mL 0.3652 mL 0.7304 mL 1.8260 mL
30 mM 0.0609 mL 0.3043 mL 0.6087 mL 1.5216 mL
40 mM 0.0456 mL 0.2282 mL 0.4565 mL 1.1412 mL
50 mM 0.0365 mL 0.1826 mL 0.3652 mL 0.9130 mL
60 mM 0.0304 mL 0.1522 mL 0.3043 mL 0.7608 mL
80 mM 0.0228 mL 0.1141 mL 0.2282 mL 0.5706 mL
100 mM 0.0183 mL 0.0913 mL 0.1826 mL 0.4565 mL
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Darunavir Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Darunavir206361-99-1TMC114 UIC-94017TMC 114TMC-114UIC94017UIC 94017UIC-94017HIVHIV ProteaseHuman immunodeficiency virusMinimalcytotoxicityAIDHIV,Inhibitorinhibitorinhibit

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