1. Anti-infection
  2. HIV
    Reverse Transcriptase
  3. Delavirdine mesylate

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

Cat. No.: HY-10571A Purity: 99.33%
Handling Instructions

Delavirdine (U 90152; BHAP-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

Delavirdine mesylate Chemical Structure

CAS No. : 147221-93-0

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Delavirdine mesylate:

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  • Biological Activity

  • Purity & Documentation

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Description

Delavirdine (U 90152; BHAP-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[1].

IC50 & Target

IC50: 0.26 μM (HIV-1 RT); 440 μM (DNA polymerase α); >550 μM (DNA polymerase δ)[1]

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].

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

In Vivo

Delavirdine (U 90152; BHAP-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].

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

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40.3 mg/mL (72.92 mM)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.33%

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Keywords:

DelavirdineU 90152BHAP-U 90152U90152U-90152HIVReverse TranscriptaseHuman immunodeficiency virusNNRTIpolymeraseHIV-1 RTAIDsDLVInhibitorinhibitorinhibit

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Delavirdine mesylate
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