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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Elvitegravir (also known as GS-9137, JTK-303, D06677 or EVG) is a potent HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively. Elvitegravir is a monoketo acid modified from the distinct diketo acid moiety (DKA) motif and is used for the treatment of HIV infection. The drug received FDA approval on August 27, 2012 for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild.
ln Vitro |
Elvitegravir (GS-9137; JTK-303; D06677) inhibits DNA strand transfer, which prevents HIV-1 cDNA integration. Elvitegravir exhibits strong anti-HIV properties against both drug-resistant clinical isolates and wild-type strains. Fascinatingly, elevategravir also demonstrates antiviral action against the simian immunodeficiency virus (SIV) and the murine leukemia virus (MLV). Three laboratory strains of HIV were effectively inhibited by elvitegravir, with EC50 values ranging from subnanomolar to nanomolar. Subsequently, Elvitegravir's efficacy was assessed in comparison to clinical isolates of wild-type HIV-1 subtypes. All HIV-1 subtypes examined with antiviral EC50s ranging from 0.1 to 1.26 nM are inhibited by elevategravir in terms of replication. Additionally, both elvitegravir and the control IN inhibitor drug L-870,810 prevented the replication of HIV-1 clinical isolates with genotypes linked to PI resistance, NRTI, and NNRTI. The MTT colorimetric test was also used to assess the cytotoxicity of these inhibitors. The average values of L-870,810 and Elvitegravir that reduced target cell viability by 50% in PBMC derived from three different donors were 2.7±0.6 μM and 4.6±0.5 μM, respectively. Elvitegravir thus suppresses a variety of HIV strains, including clinical isolates with numerous alterations linked to resistance to presently licensed antiretroviral medications and a number of HIV-1 subtypes [1].
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ln Vivo |
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Animal Protocol |
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References |
[1]. Shimura K, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74
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Molecular Formula |
C23H23CLFNO5
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Molecular Weight |
447.88
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CAS # |
697761-98-1
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Related CAS # |
Elvitegravir-d8
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SMILES |
ClC1=C([H])C([H])=C([H])C(=C1F)C([H])([H])C1C(=C([H])C2=C(C=1[H])C(C(C(=O)O[H])=C([H])N2[C@]([H])(C([H])([H])O[H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)OC([H])([H])[H]
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InChi Key |
JUZYLCPPVHEVSV-LJQANCHMSA-N
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InChi Code |
InChI=1S/C23H23ClFNO5/c1-12(2)19(11-27)26-10-16(23(29)30)22(28)15-8-14(20(31-3)9-18(15)26)7-13-5-4-6-17(24)21(13)25/h4-6,8-10,12,19,27H,7,11H2,1-3H3,(H,29,30)/t19-/m1/s1
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Chemical Name |
InChI=1S/C19H17N5O2.2CH4O3S/c20-17(21)14-2-1-13-10-16(8-5-12(13)9-1(4)26-18(25)11-3-6-15(7-4-11)24-19(22)23;2*1-5(2,3)4/h1-10H,(H3,20,21)(H4,22,23,24);2*1H3,(H,2,3,4
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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: 2.5 mg/mL (5.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.64 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.64 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 | 2.2327 mL | 11.1637 mL | 22.3274 mL | |
5 mM | 0.4465 mL | 2.2327 mL | 4.4655 mL | |
10 mM | 0.2233 mL | 1.1164 mL | 2.2327 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.