Delavirdine mesylate

Non-nucleoside reverse transcriptase inhibitor CAS# 147221-93-0

Delavirdine mesylate

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Chemical structure

Delavirdine mesylate

3D structure

Chemical Properties of Delavirdine mesylate

Cas No. 147221-93-0 SDF Download SDF
PubChem ID 441386 Appearance Powder
Formula C23H32N6O6S2 M.Wt 552.67
Type of Compound N/A Storage Desiccate at -20°C
Synonyms U 90152
Solubility DMSO : ≥ 40.3 mg/mL (72.92 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name methanesulfonic acid;N-[2-[4-[3-(propan-2-ylamino)pyridin-2-yl]piperazine-1-carbonyl]-1H-indol-5-yl]methanesulfonamide
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
Standard InChIKey MEPNHSOMXMALDZ-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H28N6O3S.CH4O3S/c1-15(2)24-19-5-4-8-23-21(19)27-9-11-28(12-10-27)22(29)20-14-16-13-17(26-32(3,30)31)6-7-18(16)25-20;1-5(2,3)4/h4-8,13-15,24-26H,9-12H2,1-3H3;1H3,(H,2,3,4)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Delavirdine mesylate

DescriptionNon-nucleoside reverse transcriptase inhibitor (NNRTI). Selectively inhibits HIV-1 reverse transcriptase (RNA-dependent DNA polymerase) over other cellular polymerases (IC50 values are 0.26, 440 and >550 μM for HIV-1 reverse transcriptase, DNA polymerase α and DNA polymerase δ). Prevents HIV-1 spread in vivo and blocks viral replication in peripheral blood lymphocytes. Orally active.

Delavirdine mesylate Dilution Calculator

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Delavirdine mesylate Molarity Calculator

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Preparing Stock Solutions of Delavirdine mesylate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.8094 mL 9.047 mL 18.094 mL 36.188 mL 45.235 mL
5 mM 0.3619 mL 1.8094 mL 3.6188 mL 7.2376 mL 9.047 mL
10 mM 0.1809 mL 0.9047 mL 1.8094 mL 3.6188 mL 4.5235 mL
50 mM 0.0362 mL 0.1809 mL 0.3619 mL 0.7238 mL 0.9047 mL
100 mM 0.0181 mL 0.0905 mL 0.1809 mL 0.3619 mL 0.4523 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Delavirdine mesylate

Delavirdine(U 90152) mesylate is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI).

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References on Delavirdine mesylate

In situ determination of delavirdine mesylate particle size in solid oral dosage forms.[Pubmed:10227710]

Pharm Res. 1999 Apr;16(4):545-8.

PURPOSE: The in-situ particle size of Delavirdine mesylate in dry mix and tablets was determined. METHODS: Optical microscopy and fluorescence microscopy combined with image analysis were used for qualitative and quantitative measurements. RESULTS: Using optical microscopy, it was demonstrated qualitatively that fragmentation of the large drug particles was occurring during tablet compression. Quantitative comparisons between dry mix and tablet samples showed that in the dry mix, drug particles remain intact, with particle lengths exceeding 200 microm. In the tablets, no particles longer than 100 microm had been observed. Analysis of multiple tablet lots revealed consistent in-situ drug particle size distributions, regardless of the original bulk drug particle size. CONCLUSIONS: Bulk drug particle size of Delavirdine mesylate is not predictive of the particle size in the tablet due to fragmentation of particles during compression. Optical and fluorescence microscopy are valuable tools for probing in-situ particle size in complex matrices.

Efficacy and safety of delavirdine mesylate with zidovudine and didanosine compared with two-drug combinations of these agents in persons with HIV disease with CD4 counts of 100 to 500 cells/mm3 (ACTG 261). ACTG 261 Team.[Pubmed:10428106]

J Acquir Immune Defic Syndr. 1999 Aug 1;21(4):281-92.

To evaluate the antiretroviral activity of Delavirdine mesylate, a non-nucleoside reverse transcriptase inhibitor of HIV-1, we performed a phase II, randomized, double-blind, multicenter trial comparing the three-drug combination of delavirdine with zidovudine and didanosine to two-drug combinations of these drugs. Patients with CD4 cell counts between 100 and 500 cells/mm3 without prior or <6 months of monotherapy with zidovudine or didanosine were randomized to one of four arms and observed on a follow-up basis for 48 weeks. In total, 544 patients were evaluated. In those assigned to the three-drug regimen, mean short-term (weeks 4-12) and long-term (weeks 40-48) change in CD4 cells from baseline were 49.3+/-8.1 and 65.4+/-13.4 cells/mm3, respectively; mean short-term and long-term HIV-1 RNA changes from baseline were -1.13 log10+/-0.12 and -0.73+/-0.12 copies/ml, respectively. These responses in CD4 cell counts and HIV-1 RNA levels were better in comparisons with each of the two-drug arms at all study points; however, differences were not consistently significant. Gastrointestinal side effects were experienced by 33% of patients (178 of 544), and 30% (121 of 407) receiving delavirdine experienced rash, only one case of which was severe. In this study, therapy with delavirdine + zidovudine + didanosine was safe and showed modest, but not always significant, antiviral activity and CD4 cell count benefit compared with two-drug regimens with these agents. Key

Multiple-Dose Pharmacokinetics of Delavirdine Mesylate and Didanosine in HIV-Infected Patients.[Pubmed:17535044]

Clin Drug Investig. 2003;23(5):323-8.

BACKGROUND: Delavirdine is a non-nucleoside reverse transcriptase inhibitor with pH-dependent absorption characteristics that has received accelerated approval for the treatment of patients with HIV-1 infection. In a prior single-dose study concurrent administration of Delavirdine mesylate and didanosine (buffered formulation) resulted in up to a 31% decrease in the area under the plasma delavirdine concentration versus time curve (AUC) compared with when both drugs were taken separately. OBJECTIVE: To evaluate the interaction of these two agents at steady state. STUDY DESIGN AND PATIENTS: A total of 11 HIV-infected subjects who were previously stabilised on didanosine were enrolled into a randomised, open-labelled crossover study. Nine subjects continued to receive their prescribed dose and schedule of didanosine, with each dose of didanosine taken either together with or 1 hour after Delavirdine mesylate (400mg every 8 hours). Pharmacokinetic studies at baseline, day 14 and day 28 were conducted and the plasma concentrations of delavirdine and didanosine were determined. RESULTS: A lower delavirdine maximum plasma concentration (C(max)) [22.4 +/- 11 vs 35.5 +/- 17muM; p = 0.045] was noted when delavirdine and didanosine were taken together. However, no significant difference was noted for delavirdine AUC (114 +/- 56 muM.h compared with 153 +/- 79 muM.h [p = 0.181]). In addition, no differences were noted for didanosine pharmacokinetic parameters between treatments. CONCLUSION: These data indicate that patients receiving didanosine and delavirdine as part of a combination regimen during long-term therapy can be instructed to take them together in an attempt to enhance adherence to treatment with both antiretroviral agents.

In vitro inhibition of human immunodeficiency virus type 1 by a combination of delavirdine (U-90152) with protease inhibitor U-75875 or interferon-alpha.[Pubmed:7528253]

J Infect Dis. 1995 Jan;171(1):61-7.

Delavirdine (bisheteroarylpiperazine, U-90152), a nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 (HIV-1), was evaluated in a two-drug combination with recombinant human interferon-alpha (IFN-alpha) or the peptidomimetic protease inhibitor U-75875 against HIV-1 replication in vitro. Viral growth was assayed in a CD4+ T cell line (H9) infected with HIVIIIB and in human peripheral blood mononuclear cells infected with the clinical isolate HIVJRCSF. Drug synergy, estimated by the combination index method and the method of Pritchard and Shipman, was observed when delavirdine was combined with U-75875 or IFN-alpha over a range of drug concentrations (delavirdine: 0.001, 0.003, 0.01, 0.03 microM; U-75875: 0.01, 0.03, 0.1, 0.3, 1.0 microM; IFN-alpha: 2, 6, 17, and 50 or 10, 30, 100, and 300 IU/mL). The combinations showed no detectable drug antagonism or cytotoxicity. These in vitro synergy data support the potential use of delavirdine with either a protease inhibitor or IFN-alpha in patients with AIDS.

U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication.[Pubmed:7685995]

Antimicrob Agents Chemother. 1993 May;37(5):1127-31.

Bisheteroarylpiperazines are potent inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). We describe a novel bisheteroarylpiperazine, U-90152 [1-(5-methanesulfonamido-1H-indol-2-yl-carbonyl)-4-[3-(1-methyl eth yl-amino)pyridinyl]piperazine], which inhibited recombinant HIV-1 RT at a 50% inhibitory concentration (IC50) of 0.26 microM (compared with IC50s of > 440 microM for DNA polymerases alpha and delta). U-90152 blocked the replication in peripheral blood lymphocytes of 25 primary HIV-1 isolates, including variants that were highly resistant to 3'-azido-2',3'-dideoxythymidine (AZT) or 2',3'-dideoxyinosine, with a mean 50% effective dose of 0.066 +/- 0.137 microM. U-90152 had low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 microM. In experiments assessing inhibition of the spread of HIV-1IIIB in cell cultures, U-90152 was much more effective than AZT. When approximately 500 HIV-1IIIB-infected MT-4 cells were mixed 1:1,000 with uninfected cells, 3 microM AZT delayed the evidence of rapid viral growth for 7 days. In contrast, 3 microM U-90152 totally prevented the spread of HIV-1, and death and/or dilution of the original inoculum of infected cells prevented renewed viral growth after U-90152 was removed at day 24. The combination of U-90152 and AZT, each at 0.5 microM, also totally prevented viral spread. Finally, although the RT amino acid substitutions K103N (lysine 103 to asparagine) and Y181C (tyrosine 181 to cysteine), which confer cross-resistance to several nonnucleoside inhibitors, also decrease the potency of U-90152, this drug retains significant activity against these mutant RTs in vitro (IC50s, approximately 8 microgramM).

Description

Delavirdine mesylate (U 90152 mesylate) is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI) of HIV-1.

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