research use only
Cat.No.S6452
| Related Targets | Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease |
|---|---|
| Other Reverse Transcriptase Inhibitors | Dapivirine (TMC120) Salicylanilide Fangchinoline Bifendate 3'-Fluoro-3'-deoxythymidine (Alovudine) Ulonivirine Lersivirine (UK-453061) 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride |
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In vitro |
DMSO
: 100 mg/mL
(180.93 mM)
Ethanol : 4 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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.
| 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 |
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| 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 | ||
| Targets/IC50/Ki |
HIV1 RT
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. |
| 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. |
References |
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