Emivirine (Synonyms: MKC-442)

Name: Emivirine
Brand: MedChemExpress
SKU: HY-15353
Rating: 4.5 (1 reviews)

Cat. No.: HY-15353 Purity: 99.73%: FAQs
Data Sheet SDS COA Handling Instructions

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Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with K_i values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity.

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

Emivirine Chemical Structure

CAS No. : 149950-60-7

Size	Price	Stock	Quantity
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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HIV HIV-1 HIV-2

Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
MT4	EC₅₀	> 10 μM Compound: MKC442, Emivirine	Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	> 100 μM Compound: MKC442, Emivirine	Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	CC₅₀	> 100 μM Compound: MKC442, Emivirine	Cytotoxicity against human MT4 cells after 96 hrs by MTT assay Cytotoxicity against human MT4 cells after 96 hrs by MTT assay	[PMID: 24805780]
MT4	CC₅₀	> 100 μM Compound: MKC-442	Protection against HIV1 HTLV 3B-induced cytopathogenicity in human MT4 cells by MTT assay Protection against HIV1 HTLV 3B-induced cytopathogenicity in human MT4 cells by MTT assay	[PMID: 17904371]
MT4	IC₅₀	0.008 μM Compound: MKC-442 emivirine	Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method	[PMID: 14643315]
MT4	EC₅₀	0.03 μM Compound: MKC442, Emivirine	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	IC₅₀	0.032 μM Compound: MKC-442 emivirine	Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method	[PMID: 14643315]
MT4	EC₅₀	0.06 μM Compound: MKC442, Emivirine	Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	0.08 μM Compound: MKC442, Emivirine	Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	IC₅₀	0.1 μM Compound: MKC-442 emivirine	Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method	[PMID: 14643315]
MT4	EC₅₀	1.5 μM Compound: MKC442, Emivirine	Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	EC₅₀	100 μM Compound: MKC442, Emivirine	Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 24805780]
MT4	CC₅₀	102 μM Compound: 33	The cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% on HIV-1 virus A012D strain The cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% on HIV-1 virus A012D strain	[PMID: 7636846]
MT4	CC₅₀	102 μM Compound: 33	The cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% on HIV-1 virus LAV-2ROD strain The cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% on HIV-1 virus LAV-2ROD strain	[PMID: 7636846]
MT4	CC₅₀	186 μM Compound: 33	Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50% Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50%	[PMID: 7636846]
PBL	CC₅₀	90 μM Compound: 33	The cytotoxic concentration of compound required to reduce the viability of mock-infected PBL cells by 50% on HIV-1 virus HTLV-IIIB strain The cytotoxic concentration of compound required to reduce the viability of mock-infected PBL cells by 50% on HIV-1 virus HTLV-IIIB strain	[PMID: 7636846]

In Vitro

Emivirine (EMV) is also specific for HIV-1 RT and was without effect on HIV-2^[2].
Emivirine (EMV) has no obvious toxicity for human healthy cells^[2].

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

Cell Viability Assay^[2]

Cell Line:	Human bone marrow cells collected from normal healthy volunteers.
Concentration:	0, 0.1, 1, 10, or 100 μM.
Incubation Time:	14 days.
Result:	At concentrations of 0.1 to 10 μM, no effect on cell growth, lactic acid production, mitochondrial DNA synthesis, or mitochondrial structure was seen compared to what occurred with untreated HepG2 cells.

In Vivo

Tthe approximate lethal oral dose of Emivirine (EMV) for rats was ≥3 g/kg for males and 2.5 g/kg for females^[2].

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

Animal Model:	Male Sprague-Dawley rats^[2].
Dosage:	50 mg/kg.
Administration:	Gavage.
Result:	The oral absorption was 68%.

Clinical Trial

Molecular Weight

302.37

Formula

C₁₇H₂₂N₂O₃

CAS No.

149950-60-7

Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(C(C(C)C)=C(CC2=CC=CC=C2)N1COCC)=O

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 (330.72 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	3.3072 mL	16.5360 mL	33.0721 mL
5 mM	0.6614 mL	3.3072 mL	6.6144 mL
10 mM	0.3307 mL	1.6536 mL	3.3072 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (8.27 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 (8.27 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)

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: 99.73%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (252 KB) HNMR (248 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Panita Decha, et al. Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions. J Enzyme Inhib Med Chem. 2011 Feb;26(1):29-36. [Content Brief]

[2]. G M Szczech, et al. Safety assessment, in vitro and in vivo, and pharmacokinetics of emivirine, a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2000 Jan;44(1):123-30 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3072 mL	16.5360 mL	33.0721 mL	82.6802 mL
	5 mM	0.6614 mL	3.3072 mL	6.6144 mL	16.5360 mL
	10 mM	0.3307 mL	1.6536 mL	3.3072 mL	8.2680 mL
	15 mM	0.2205 mL	1.1024 mL	2.2048 mL	5.5120 mL
	20 mM	0.1654 mL	0.8268 mL	1.6536 mL	4.1340 mL
	25 mM	0.1323 mL	0.6614 mL	1.3229 mL	3.3072 mL
	30 mM	0.1102 mL	0.5512 mL	1.1024 mL	2.7560 mL
	40 mM	0.0827 mL	0.4134 mL	0.8268 mL	2.0670 mL
	50 mM	0.0661 mL	0.3307 mL	0.6614 mL	1.6536 mL
	60 mM	0.0551 mL	0.2756 mL	0.5512 mL	1.3780 mL
	80 mM	0.0413 mL	0.2067 mL	0.4134 mL	1.0335 mL
	100 mM	0.0331 mL	0.1654 mL	0.3307 mL	0.8268 mL

Emivirine Related Classifications

Inflammation/Immunology Infection

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:

Emivirine149950-60-7MKC-442MKC442MKC 442HIVHuman immunodeficiency virusHepG2HIV-1NNRTInucleosidereversetranscriptaseInhibitorinhibitorinhibit

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Emivirine (Synonyms: MKC-442)

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Complete Stock Solution Preparation Table

Emivirine Related Classifications

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