Delavirdine mesylate (Synonyms: U 90152 mesylate; BHAP-U 90152 mesylate)

Name: Delavirdine mesylate
Brand: MedChemExpress
SKU: HY-10571A
Rating: 5.0 (3 reviews)

Cat. No.: HY-10571A Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

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Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC₅₀=0.26?μM) over DNA polymerase?α?(IC₅₀=440 μM) and polymerase?δ (IC₅₀>550?μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.

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

Delavirdine mesylate Chemical Structure

CAS No. : 147221-93-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 50	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 50	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 41	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Delavirdine mesylate:

Delavirdine Get quote

3 Publications Citing Use of MCE Delavirdine mesylate

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HIV HIV-1 HIV-2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
CEM-SS	ED₅₀	0.06 μM Compound: delavirdine mesylate	Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay	[PMID: 15217281]
MT4	EC₅₀	> 28.23 μM Compound: DLV	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay	[PMID: 26994843]
MT4	CC₅₀	> 36 μM Compound: DLV	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 25707013]
MT4	CC₅₀	> 36 μM Compound: DLV	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 25626145]
MT4	EC₅₀	> 36 μM Compound: DLV	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25707013]
MT4	EC₅₀	> 36 μM Compound: DLV	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25626145]
MT4	CC₅₀	> 36 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 24239481]
MT4	EC₅₀	> 36 μM Compound: DLV	Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	[PMID: 24239481]
MT4	CC₅₀	> 36.19 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 22591854]
MT4	EC₅₀	> 36.19 μM Compound: DLV	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22591854]
MT4	CC₅₀	> 36.2 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 22405288]
MT4	EC₅₀	> 36.2 μM Compound: DLV	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	[PMID: 22405288]
MT4	EC₅₀	> 43.81 μM Compound: DLV	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 25240095]
MT4	CC₅₀	> 43.81 μM Compound: DLV	Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay	[PMID: 25240095]
MT4	EC₅₀	0.027 μM Compound: DLV	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay	[PMID: 26994843]
MT4	EC₅₀	0.06 μM Compound: DLV (Mesylate)	Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 21872971]
MT4	EC₅₀	0.13 μM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	[PMID: 24239481]
MT4	EC₅₀	0.54 μM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25707013]
MT4	EC₅₀	0.66 μM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 25240095]
MT4	EC₅₀	1.72 μM Compound: DLV (Mesylate)	Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 21872971]
MT4	EC₅₀	2.23 μM Compound: DLV (Mesylate)	Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 21872971]
MT4	CC₅₀	28.23 μM Compound: DLV	Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay	[PMID: 26994843]
MT4	CC₅₀	30.4 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 28254696]
MT4	EC₅₀	32.6 nM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	[PMID: 22405288]
MT4	EC₅₀	35.01 nM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22591854]
MT4	EC₅₀	540 nM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25626145]

In Vitro

Delavirdine has an 50% cytotoxicity at concentrations >100 μM in H9 and PBMC cultures.Delavirdine has low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 μM^[1].
Delavirdine inhibits HIV-1 reverse transcriptase (RT) wild type with an IC₅₀ value of 0.26?μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC₅₀ values of 8.32 uM and 7.7 uM, respectively^[1].

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

In Vivo

Delavirdine (U 90152) mesylate (oral gavage; 10 mg/kg, 200 mg/kg, 250 mg/kg; single dose) is absorbed and metabolized rapidly, that it constitutes a minor component in circulation, that its pharmacokinetics are nonlinear, and that its metabolism to desalkyl delavirdine is capacity limited or inhibitable in CD-1 mice (PK study)^[1].

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

Clinical Trial

Molecular Weight

552.67

Formula

C₂₃H₃₂N₆O₆S₂

CAS No.

147221-93-0

Appearance

Solid

Color

White to yellow

SMILES

O=S(NC1=CC=C(NC(C(N2CCN(C3=C(NC(C)C)C=CC=N3)CC2)=O)=C4)C4=C1)(C)=O.O=S(O)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 40.3 mg/mL (72.92 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	1.8094 mL	9.0470 mL	18.0940 mL
5 mM	0.3619 mL	1.8094 mL	3.6188 mL
10 mM	0.1809 mL	0.9047 mL	1.8094 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 (sealed storage, away from moisture). 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 (4.52 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 (4.52 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.52 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (9.05 mM); Suspended solution; Need ultrasonic

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.82%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (254 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Dueweke TJ, et al. U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication. Antimicrob Agents Chemother. 1993 May;37(5):1127-31. [Content Brief]

[2]. Mayland Chang, et al. Metabolism of the HIV-1 Reverse Transcriptase Inhibitor Delavirdine In Mice. Research Article

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8094 mL	9.0470 mL	18.0940 mL	45.2350 mL
	5 mM	0.3619 mL	1.8094 mL	3.6188 mL	9.0470 mL
	10 mM	0.1809 mL	0.9047 mL	1.8094 mL	4.5235 mL
	15 mM	0.1206 mL	0.6031 mL	1.2063 mL	3.0157 mL
	20 mM	0.0905 mL	0.4523 mL	0.9047 mL	2.2617 mL
	25 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8094 mL
	30 mM	0.0603 mL	0.3016 mL	0.6031 mL	1.5078 mL
	40 mM	0.0452 mL	0.2262 mL	0.4523 mL	1.1309 mL
	50 mM	0.0362 mL	0.1809 mL	0.3619 mL	0.9047 mL
	60 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7539 mL

Delavirdine mesylate Related Classifications

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:

Delavirdine147221-93-0U 90152BHAP-U 90152U90152U-90152HIVReverse TranscriptaseHuman immunodeficiency virusNNRTIpolymeraseHIV-1 RTAIDsDLVInhibitorinhibitorinhibit

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Delavirdine mesylate (Synonyms: U 90152 mesylate; BHAP-U 90152 mesylate)

Customer Review

Other Forms of Delavirdine mesylate:

Delavirdine mesylate Related Antibodies

3 Publications Citing Use of MCE Delavirdine mesylate

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIV Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Delavirdine mesylate Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Delavirdine mesylate Related Classifications

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