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Purity: ≥98%
Delavirdine mesylate (U-90152) is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor (NNRTI) of HIV-1 used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. Although delavirdine was approved by the U.S. Food and Drug Administration in 1997, its efficacy is lower than other NNRTIs, especially efavirenz, and it also has an inconvenient schedule. These factors have led the U.S. DHHS not to recommend its use as part of initial therapy.
| ln Vitro |
Delavirdine was 50% cytotoxic in H9 and PBMC cells at doses greater than 100 μM. At 100 μM, delavirdine causes less than 8% reduction in peripheral blood lymphocyte viability, indicating its modest cytotoxicity [1]. With an IC50 value of 0.26 μM, delavirdine inhibits HIV-1 reverse transcriptase (RT) in its wild-type form. It also inhibits RT replaced with Y181C and K103N, with IC50 values of 8.32 uM and 7.7 uM, respectively [1].
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| ln Vivo |
Delavirdine (U 90152) mesylate is a small circulating component that is quickly absorbed and digested. It is administered orally as a single dosage at 10 mg/kg, 200 mg/kg, or 250 mg/kg. Its capacity to metabolize to dealkylavirdine is restricted or hindered in CD-1 mice (PK research), and its metabolic kinetics are non-linear [1].
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| 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.
[2]. Mayland Chang, et al. Metabolism of the HIV-1 Reverse Transcriptase Inhibitor Delavirdine In Mice. Research Article |
| Molecular Formula |
C22H28N6O3S.CH4O3S
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| Molecular Weight |
552.66678
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| CAS # |
147221-93-0
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| Related CAS # |
Delavirdine;136817-59-9
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| 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
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| Synonyms |
Rescriptor; BHAP-U 90152; U-90152; BHAP U 90152; U90152; BHAP-U-90152; U 90152; DLV
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 40.3 mg/mL (~72.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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