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| 25mg |
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Purity: ≥98%
Nevirapine (also known as NSC 641530; BI-RG 587; NSC 641530; NVP) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV-1 infection and AIDS. It inhibits HIV-1 reverse transcriptase with a Ki of 270 μM. As with other antiretroviral drugs, HIV rapidly develops resistance if nevirapine is used alone, so recommended therapy consists of combinations of three or more antiretrovirals. Nevirapine in triple combination therapy has been shown to suppress viral load effectively when used as initial antiretroviral therapy.
| ln Vitro |
Only CYP3A4 is inhibited by nevirapine at values far above those that are therapeutically relevant (Ki=270 μM)[1]. Nevirapine has been applied to tumors in a number of human cancer models as a re-differentiation agent. After 48 hours of treatment, nevirapine strongly reduces cell growth at all tested dosages (100, 200, 350, and 500 μM). Nevirapine dramatically raises the proportion of apoptotic cells when compared to control at a high dose (500 μM)[2]. In multiple cellular assays, nevirapine is a strong and specific inhibitor (IC50=10-100 nM) of the replication of a broad range of HIV-1 strains[3].
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| ln Vivo |
Nevirapine can be used with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., didanosine, zidovudine, etc.) in combination. The FDA has approved the use of nevirapine in conjunction with HIV-1 protease inhibitors, such as saquinavir, ritonavir, indinavir, and so forth. In humans, 2-, 3-, 8-, and 12-hydroxynevirapine glucuronide conjugates are the main way that nevirapine is excreted in the urine[1]. All sexes of mice, rats, rabbits, monkeys, and chimpanzees fully absorb nevirapine. In all investigated animal species, nevirapine is substantially metabolized in both sexes[4]. When compared to the control, nevirapine (9 mg/kg, 18 mg/kg, and 36 mg/kg) significantly reduces the ulcer severity score and ulcer index[5].
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| References |
[1]. Erickson DA, et al. Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitornevirapine by human hepatic cytochromes P-450. Drug Metab Dispos. 1999 Dec;27(12):1488-95.
[2]. Dong JJ, et al. In vitro evaluation of the therapeutic potential of nevirapine in treatment of human thyroid anaplastic carcinoma. Mol Cell Endocrinol. 2013 May 6;370(1-2):113-8. [3]. Merluzzi VJ, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science. 1990 Dec 7;250(4986):1411-3. [4]. Riska PS, et al. Biotransformation of nevirapine, a non-nucleoside HIV-1 reverse transcriptase inhibitor, in mice, rats, rabbits, dogs, monkeys, and chimpanzees. Drug Metab Dispos. 1999 Dec;27(12):1434-47. [5]. Onasanwo SA, et al. Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats. Afr J Med Med Sci. 2015 Sep;44(3):251-9 |
| Molecular Formula |
C15H14N4O
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|---|---|
| Molecular Weight |
266.3
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| CAS # |
129618-40-2
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| Related CAS # |
Nevirapine-d4;1051418-95-1;Nevirapine-d3;1051419-24-9
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| SMILES |
O=C1C2=CC=CN=C2N(C3CC3)C4=NC=CC(C)=C4N1
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| InChi Key |
NQDJXKOVJZTUJA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14N4O/c1-9-6-8-17-14-12(9)18-15(20)11-3-2-7-16-13(11)19(14)10-4-5-10/h2-3,6-8,10H,4-5H2,1H3,(H,18,20)
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| Chemical Name |
11-cyclopropyl-4-methyl-5,11-dihydro-6H-dipyrido[3,2-b:2,3-e][1,4]diazepin-6-one
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| Synonyms |
NSC 641530; BI-RG-587; BIRG 0587; BIRG587; HSDB 7164; Nevirapine; NSC 641530; NVP; trade name: Viramune; Viramune XR.
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (5.37 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 14.3 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: ≥ 1.43 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7552 mL | 18.7758 mL | 37.5516 mL | |
| 5 mM | 0.7510 mL | 3.7552 mL | 7.5103 mL | |
| 10 mM | 0.3755 mL | 1.8776 mL | 3.7552 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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