2. Anti-infection
  3. HIV Reverse Transcriptase
  4. Doravirine

Doravirine  (Synonyms: MK-1439)

製品番号: HY-16767 純度: 99.79%
COA 取扱説明書 Technical Support

Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.

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Doravirine

Doravirine 構造式

CAS 番号 : 1338225-97-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 145 在庫あり
Solution
10 mM * 1 mL in DMSO USD 145 在庫あり
Solid
5 mg $132 在庫あり
10 mg $220 在庫あり
25 mg $429 在庫あり
50 mg $660 在庫あり
100 mg $990 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 13 publication(s) in Google Scholar

Other Forms of Doravirine:

Doravirine 関連抗体

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製品説明

Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively[1].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
MT4 CC50
>293 3
Compound: DOR
Cytotoxicity against human MT4 cells
Cytotoxicity against human MT4 cells
[PMID: 35061384]
MT4 CC50
> 294 3
Compound: DOR
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
[PMID: 34496571]
MT4 CC50
293.24 3
Compound: DOR
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
[PMID: 35797898]
MT4 CC50
> 294 3
Compound: 6; DOR
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
[PMID: 30606670]
MT4 CC50
293.24 3
Compound: DOR
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
[PMID: 35797898]
MT4 CC50
293.24 3
Compound: DOR
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
[PMID: 35797898]
MT4 CC50
>294 3
Compound: 6; DOR
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
[PMID: 30606670]
MT4 CC50
> 293 3
Compound: DOR
Cytotoxicity against human MT4 cells
Cytotoxicity against human MT4 cells
[PMID: 35061384]
MT4 CC50
>294 3
Compound: DOR
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
[PMID: 34496571]
MT4 CC50
> 294 3
Compound: 6; DOR
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
[PMID: 30606670]
MT4 CC50
> 294 3
Compound: DOR
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
[PMID: 34496571]
MT4 CC50
> 294 3
Compound: DOR
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
[PMID: 38613773]
体外実験

Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitors with minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses)[1].

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

Doravirine 関連抗体
体内実験

Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

425.75

分子式

C17H11ClF3N5O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC(OC2=C(C(F)(F)F)C=CN(CC(N3C)=NNC3=O)C2=O)=CC(Cl)=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (234.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3488 mL 11.7440 mL 23.4880 mL
5 mM 0.4698 mL 2.3488 mL 4.6976 mL
10 mM 0.2349 mL 1.1744 mL 2.3488 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.

  • Molarity Calculator

  • 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)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (5.87 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
純度とドキュメンテーション
参考文献

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 2.3488 mL 11.7440 mL 23.4880 mL 58.7199 mL
5 mM 0.4698 mL 2.3488 mL 4.6976 mL 11.7440 mL
10 mM 0.2349 mL 1.1744 mL 2.3488 mL 5.8720 mL
15 mM 0.1566 mL 0.7829 mL 1.5659 mL 3.9147 mL
20 mM 0.1174 mL 0.5872 mL 1.1744 mL 2.9360 mL
25 mM 0.0940 mL 0.4698 mL 0.9395 mL 2.3488 mL
30 mM 0.0783 mL 0.3915 mL 0.7829 mL 1.9573 mL
40 mM 0.0587 mL 0.2936 mL 0.5872 mL 1.4680 mL
50 mM 0.0470 mL 0.2349 mL 0.4698 mL 1.1744 mL
60 mM 0.0391 mL 0.1957 mL 0.3915 mL 0.9787 mL
80 mM 0.0294 mL 0.1468 mL 0.2936 mL 0.7340 mL
100 mM 0.0235 mL 0.1174 mL 0.2349 mL 0.5872 mL
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Doravirine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Doravirine1338225-97-0MK-1439MK1439MK 1439HIVReverse TranscriptaseHuman immunodeficiency virusInhibitorinhibitorinhibit

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製品名:
Doravirine
製品番号:
HY-16767
数量:
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