Home Microbiology Reverse Transcriptase inhibitor Delavirdine mesylate

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Delavirdine mesylate Reverse Transcriptase inhibitor

Cat.No.S6452

Delavirdine Mesylate(U 90152 mesylate) is a mesylate salt form of delavirdine, which is a synthetic, non-nucleoside reverse transcriptase inhibitor.
Delavirdine mesylate Reverse Transcriptase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 552.67

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S645201 DMSO]100 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.84%
99.84

Chemical Information, Storage & Stability

Molecular Weight 552.67 Formula

C23H32N6O6S2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 147221-93-0 -- Storage of Stock Solutions

Synonyms U 90152 mesylate Smiles CC(C)NC1=C(N=CC=C1)N2CCN(CC2)C(=O)C3=CC4=C(N3)C=CC(=C4)NS(=O)(=O)C.CS(=O)(=O)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (180.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
HIV1 RT [1]
0.26 μM
In vitro

Delavirdine is a potent and selective inhibitor of the HIV-1 RT (IC50=0.26 μM verus IC50s>440 μM for pol alpha and delta). Delavirdine has low cellular cytotoxicity, causing less than 8% reduction in human lymphocyte viability at 100 μM[1].
In vivo

Following single dose administration, the pharmacokinetics of delavirdine is nonlinear in rats, and appeared to be nonlinear in dogs. Systemic clearances in the dog, at a dose of 10 mg/kg, are approximately 20-fold lower than in the rat, whereas the clearances in monkeys are comparable to those in rats. Absolute p.o. bioavailabilities increase in the order monkey (30%) < rat (65%) < dog (100%) when equivalent i.v. and p.o. doses are administered[1].
References

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