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| 100mg |
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| 1g |
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Purity: ≥98%
Efavirenz (also called Sustiva, Stocrin, DMP-266, DMP 266), a non-nucleoside reverse transcriptase inhibitor (NNRTI), is a highly potent and specific inhibitor of human immunodeficiency virus type 1 reverse transcriptase with Ki value of 2.93nM. Efavirenz was approved by the FDA in 1998. It is usually used in a combination therapy with other antiretroviral drugs. Efavirenz is a potent inhibitor of both wild-type HIV-1 RT and HIV-1 variants which express series of NNRTI resistance-associated amino acid substitutions.
| ln Vitro |
It is discovered that efavirenz (L-743726) may suppress a panel of mutant viruses resistant to nonnucleoside reverse transcriptase inhibitors (NNRTIs) that express a single RT amino acid substitution, with 95% inhibitory doses of ≤ 1.5μM. When efavirenz is examined for its ability to inhibit different polymerase enzymes, it is discovered that it lacks activity (IC50>300μM). Several wild-type T-lymphoid cell line-adapted variations are efficiently inhibited by efavirenz. In primary lymphoid and monocytoid cell cultures, wild-type primary isolates of the virus exhibit the same activity (IC95, 1.5 to 3.0 nM). Furthermore, HIV-1 genotypes that contain RT amino acid changes, which confer resistance to other NNRTIs, are effectively inhibited by efavirenz. for comparative purposes [1]. With an IC50 of 60 nM, efavirenz is a non-nucleoside analog reverse transcriptase inhibitor (NNRTI)[2]. With an IC50 of 17 nM, efavirenz inhibits synthesis utilizing an RNA PPT-primed substrate[3].
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| ln Vivo |
Efavirenz (L-743726) is eliminated from rats quickly after intravenous injection, but it is eliminated from monkeys much more slowly. In both species, the large volume of distribution (two to four times the body water content) suggests extensive tissue binding. Rats have a 16% oral bioavailability. After giving an intravenous dose of 1 mg/kg of Efavirenz, the half-life in monkeys was more than 2.5 hours. Orally, efavirenz is well absorbed. Plasma levels are consistently high when oral doses administered as fine suspensions in 0.5% aqueous methylcellulose are given to monkeys. Approximately 3.0 hours after a dose of 2.0 mg/kg, peak levels of 0.5μM are achieved. According to estimates, the absolute bioavailability is 42%. A plasma peak level of 3.22 μM is obtained with a dose of 10 mg/kg. One chimpanzee received an oral dose of 10 mg/kg, which resulted in plasma concentrations of 4.12, 2.95, and 2.69 μM at 2, 8, and 24 hours after dosing, respectively[1].
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| References |
[1]. Young SD, et al. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1995 Dec;39(12):2602-5.
[2]. Held DM, et al. Differential susceptibility of HIV-1 reverse transcriptase to inhibition by RNA aptamers in enzymatic reactions monitoring specific steps during genome replication. J Biol Chem. 2006 Sep 1;281(35):25712-22. [3]. Grobler JA, et al. HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. J Biol Chem. 2007 Mar 16;282(11):8005-10 |
| Molecular Formula |
C14H9CLF3NO2
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|---|---|
| Molecular Weight |
315.67
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| CAS # |
154598-52-4
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| Related CAS # |
(Rac)-Efavirenz-d4;1246812-58-7;Efavirenz-d5;1132642-95-5;Efavirenz-13C6;1261394-62-0
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| SMILES |
C1CC1C#C[C@]2(C3=C(C=CC(=C3)Cl)NC(=O)O2)C(F)(F)F
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| InChi Key |
XPOQHMRABVBWPR-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C14H9ClF3NO2/c15-9-3-4-11-10(7-9)13(14(16,17)18,21-12(20)19-11)6-5-8-1-2-8/h3-4,7-8H,1-2H2,(H,19,20)/t13-/m0/s1
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| Chemical Name |
(4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one
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| Synonyms |
DMP-266, DMP 266; Efavirenz; Sustiva; Stocrin; DMP-266; DMP 266; trade name: efavirenz; L-743,726; L-743726; DMP266; EFV; L 743726
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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: ≥ 2.08 mg/mL (6.59 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 20.8 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: ≥ 2.08 mg/mL (6.59 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 20.8 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: ≥ 2.08 mg/mL (6.59 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 | 3.1679 mL | 15.8393 mL | 31.6787 mL | |
| 5 mM | 0.6336 mL | 3.1679 mL | 6.3357 mL | |
| 10 mM | 0.3168 mL | 1.5839 mL | 3.1679 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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