Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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E135556-10mg | 10mg | In stock | $58.90 | |
E135556-50mg | 50mg | In stock | $98.90 | |
E135556-250mg | 250mg | In stock | $445.90 | |
E135556-1g | 1g | In stock | $1,603.90 | |
E135556-5g | 5g | In stock | $7,217.90 |
Non-nucleoside reverse transcriptase inhibitor
Synonyms | efavirenz | 154598-52-4 | Sustiva | Stocrin | DMP-266 | DMP 266 | (-)-Efavirenz | EFV | (4S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one | L-743726 | Viraday | Efavirenz teva | (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl) |
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Specifications & Purity | Moligand™, ≥98%(HPLC) |
Biochemical and Physiological Mechanisms | Efavirenz is a nonnucleoside reverse transcriptase inhibitor (NNRTI). It is an anti-HIV drug, commonly used in combination therapy for AIDs treatment. It is part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Human immunodeficiency virus type 1 reverse transcriptase inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI). |
ALogP | 4 |
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IUPAC Name | (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-1H-3,1-benzoxazin-2-one |
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INCHI | 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 |
InChi Key | XPOQHMRABVBWPR-ZDUSSCGKSA-N |
Canonical SMILES | C1CC1C#CC2(C3=C(C=CC(=C3)Cl)NC(=O)O2)C(F)(F)F |
Isomeric SMILES | C1CC1C#C[C@]2(C3=C(C=CC(=C3)Cl)NC(=O)O2)C(F)(F)F |
WGK Germany | 3 |
PubChem CID | 64139 |
Molecular Weight | 315.67 |
CAS Registry No. | 154598-52-4 |
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PubChem CID | 64139 |
ChEMBL Ligand | CHEMBL223228 |
BindingDB Ligand | 2483 |
DrugBank Ligand | DB00625 |
RCSB PDB Ligand | EFZ |
DrugCentral Ligand | 989 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
F2217252 | Certificate of Analysis | Apr 02, 2024 | E135556 |
F2213221 | Certificate of Analysis | Mar 20, 2024 | E135556 |
L2109529 | Certificate of Analysis | Sep 21, 2023 | E135556 |
L2109531 | Certificate of Analysis | Sep 21, 2023 | E135556 |
L2109533 | Certificate of Analysis | Sep 21, 2023 | E135556 |
H1513112 | Certificate of Analysis | Mar 15, 2023 | E135556 |
E135556-50mg;G2006052 | Certificate of Analysis | May 11, 2022 | E135556 |
E135556-250mg;G2006050 | Certificate of Analysis | May 11, 2022 | E135556 |
Solubility | Insoluble in water; Very soluble in Methanol,Ethanol |
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Sensitivity | heat sensitive |
Specific Rotation[α] | -95° (C=1,MeOH) |
Melt Point(°C) | 138 °C |
Pictogram(s) | GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H319:Causes serious eye irritation H302:Harmful if swallowed H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child |
Precautionary Statements | P273:Avoid release to the environment. P501:Dispose of contents/container to ... |
WGK Germany | 3 |
Merck Index | 3521 |
1. Hesse LM, von Moltke LL, Shader RI, Greenblatt DJ. (2001) Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion.. Drug Metab Dispos, 29 (2): (100-2). [PMID:11159797] |
2. von Moltke LL, Greenblatt DJ, Granda BW, Giancarlo GM, Duan SX, Daily JP, Harmatz JS, Shader RI. (2001) Inhibition of human cytochrome P450 isoforms by nonnucleoside reverse transcriptase inhibitors.. J Clin Pharmacol, 41 (1): (85-91). [PMID:11225565] |
3. Decloedt EH, Rosenkranz B, Maartens G, Joska J. (2015) Central nervous system penetration of antiretroviral drugs: pharmacokinetic, pharmacodynamic and pharmacogenomic considerations.. Clin Pharmacokinet, 54 (6): (581-98). [PMID:25777740] |
4. Wang PF, Neiner A, Kharasch ED. (2019) Efavirenz Metabolism: Influence of Polymorphic CYP2B6 Variants and Stereochemistry.. Drug Metab Dispos, 47 (10): (1195-1205). [PMID:31324697] |
5. Fernández-Bargiela N, Rotea-Salvo S, Margusino-Framiñán L, Balboa-Barreiro V, Martín-Herranz I, Castro-Iglesias Á, Mena-De-Cea Á, López-Calvo S, Vázquez-Rodríguez P, Míguez-Rey E et al.. (2020) Discontinuation due to neuropsychiatric adverse events with efavirenz- and dolutegravir-based antiretroviral therapy: a comparative real-life study.. Eur J Hosp Pharm, 129 (3): (589-97). [PMID:33051194] |
6. Young SD, Britcher SF, Tran LO, Payne LS, Lumma WC, Lyle TA, Huff JR, Anderson PS, Olsen DB, Carroll SS et al.. (1995) L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase.. Antimicrob Agents Chemother, 39 (12): (2602-5). [PMID:8592986] |