Cat. No.: HY-10571A

Delavirdine mesylate

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

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

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.

Purity: 99.73%
CAS No.: 147221-93-0
Formula: C₂₃H₃₂N₆O₆S₂
Molecular Weight:552.67

Storage:

4°C, sealed storage, away from moisture

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

Delavirdine mesylate Chemical Structure

CAS No.: 147221-93-0

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

HIV-1

All HIV Isoforms :

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	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	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	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	>36.19 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	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	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	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	>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	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	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	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	>36.19 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	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	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	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]
MT4	IC₅₀	0.063 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 190A strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 190A strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	0.063 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from LAI strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from LAI strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	0.158 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 101E strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 101E strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	1.26 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 188L strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 188L strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	1.59 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 106A strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 106A strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	2 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 181C strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 181C strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	2.51 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 100I strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 100I strain of HIV-1 virus	[PMID: 11527703]
MT4	IC₅₀	2.51 μM Compound: Delavirdine	Compound was tested for potency to achieve protection of MT-4 cells from 103N strain of HIV-1 virus Compound was tested for potency to achieve protection of MT-4 cells from 103N strain of HIV-1 virus	[PMID: 11527703]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 147221-93-0
Appearance Solid
Molecular Weight 552.67
Formula C₂₃H₃₂N₆O₆S₂
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
Synonyms

U 90152 mesylate; BHAP-U 90152 mesylate
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)

Publications (3)

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Journal Impact Factor

Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Sci Rep

NMR characterization of HIV-1 reverse transcriptase binding to various non-nucleoside reverse transcriptase inhibitors with different activities. [Abstract]

2015 Oct 29;5:15806. PMID: 26510386
Future Med Chem

Discovery of CDK4 inhibitors by convolutional neural networks. [Abstract]

2019 Feb;11(3):165-177. PMID: 30556417

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (180.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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
	80 mM	0.0226 mL	0.1131 mL	0.2262 mL	0.5654 mL
	100 mM	0.0181 mL	0.0905 mL	0.1809 mL	0.4523 mL

Keywords

Delavirdine mesylate

3 Cited Publications

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Delavirdine mesylate

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All HIV Isoforms

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Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Delavirdine mesylate

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Delavirdine mesylate

All HIV Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Delavirdine mesylate Related Classifications

Cat. No.: HY-10571A