| Size | Price | Stock | Qty |
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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%
| Targets |
HIV-1
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|---|---|
| ln Vitro |
With an IC50 of 7.5± 0.3 nM, bictegravir (BIC) inhibits the strand transfer activity. With an IC50 of 241±51 nM, bictegravir is a much weaker inhibitor of HIV-1 IN's 3′-processing activity than it is of strand transfer activity. In comparison to the mock-treated control, bictegravir increases the accumulation of 2-LTR circles by approximately five times and decreases the quantity of real integration products in infected cells by a factor of 100. With EC50s of 1.5 and 2.4 nM, respectively, bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells. With EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, bictegravir demonstrates strong antiviral effects in primary CD4+ T lymphocytes and monocyte-derived macrophages. These values are in line with those observed in T-cell lines.
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| ln Vivo |
HIV-1 IIIb is cultured in bulk on MT-2 cells for three hours at 37°C, with a cell density of 2×106 cells/mL. Bictegravir (BIC) or DMSO (mock-treated control) are given to infected MT-2 cells at a final concentration that is at least 20 times the antiviral 50% effective concentration (EC50) of each drug.The cells are harvested for total DNA isolation after these plates are incubated at 37°C for either 12 hours (for late reverse transcription product quantification) or 24 hours (for 2-LTR circle and Alu-LTR product quantification). Using the DNA minikit, DNA is extracted from each well and collected as a 100-μL eluate. The host globin gene level in each sample is used to normalize TaqMan real-time PCR-quantified 2-LTR junctions (2-LTR circles), late reverse transcription products, and integration junctions (Alu-LTR)[1].
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| Cell Assay |
In bulk culture, MT-2 cells are infected with HIV-1 IIIb for three hours at 37°C at a cell density of 2×106 cells/mL. Bictegravir (BIC) or DMSO (mock-treated control) are given to infected MT-2 cells at a final concentration that is at least 20 times the antiviral 50% effective concentration (EC50) of each drug. The cells are harvested for total DNA isolation after these plates are incubated at 37°C for either 12 hours (for late reverse transcription product quantification) or 24 hours (for 2-LTR circle and Alu-LTR product quantification).Using the DNA minikit, DNA is extracted from each well and collected as a 100-μL eluate. The host globin gene level in each sample serves as the standard for TaqMan real-time PCR quantification of 2-LTR junctions (2-LTR circles), late reverse transcription products, and integration junctions (Alu-LTR)[1].
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| References |
[1]. Antimicrob Agents Chemother.2016 Nov 21;60(12):7086-7097.
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| Molecular Formula |
C21H18F3N3O5
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|---|---|---|
| Molecular Weight |
449.37
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| Exact Mass |
449.12
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| Elemental Analysis |
C, 56.13; H, 4.04; F, 12.68; N, 9.35; O, 17.80
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| CAS # |
1611493-60-7
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| Related CAS # |
Bictegravir sodium;1807988-02-8;Bictegravir-15N,d2
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| Appearance |
Solid powder
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| SMILES |
O=C(C1=CN(C2=C(O)C1=O)C[C@@]3([H])O[C@](C4)([H])CC[C@]4([H])N3C2=O)NCC5=C(F)C=C(F)C=C5 F
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| InChi Key |
SOLUWJRYJLAZCX-LYOVBCGYSA-N
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| InChi Code |
InChI=1S/C21H18F3N3O5/c22-9-3-14(23)12(15(24)4-9)6-25-20(30)13-7-26-8-16-27(10-1-2-11(5-10)32-16)21(31)17(26)19(29)18(13)28/h3-4,7,10-11,16,29H,1-2,5-6,8H2,(H,25,30)/t10-,11+,16+/m0/s1
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| Chemical Name |
(2R,5S,13aR)-8-hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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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) |
DMSO : 83.3 ~90 mg/mL ( 185.37 ~200.27 mM）
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.56 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 (5.56 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 (5.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.56 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 5: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (5.56 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2253 mL | 11.1267 mL | 22.2534 mL | |
| 5 mM | 0.4451 mL | 2.2253 mL | 4.4507 mL | |
| 10 mM | 0.2225 mL | 1.1127 mL | 2.2253 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.
Resistance profile of BIC and other INSTIs against 47 HIV-1 patient-derived isolates with INSTI resistance mutations.Antimicrob Agents Chemother. 2016 Dec; 60(12): 7086–7097. |
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Progress of BIC, DTG, and EVG resistance selection with HIV-1 IIIb.Antimicrob Agents Chemother. 2016 Dec; 60(12): 7086–7097. |
HIV-1 IIIb resistance breakthrough in MT-2 cells. Viral resistance breakthrough for each drug was tested in four independent infected cultures in the presence of constant drug pressure for up to 35 days.Antimicrob Agents Chemother. 2016 Dec; 60(12): 7086–7097. |
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