Bictegravir-15N,d2
Based on 1 Customer Validation
Bictegravir-15N,d2 (GS-9883-15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605). Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
For research use only. We do not sell to patients.
- Purity: 96.09%
- Formula: C21H16D2F3N215NO5
- Molecular Weight:452.39
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 7.5 nM (HIV-1 integrase)[1]
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Bictegravir (BIC) inhibits the strand transfer activity with an IC50 of 7.5± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 1611493-60-7
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Appearance Solid
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Molecular Weight 452.39
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Formula C21H16D2F3N215NO5
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Color White to off-white
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SMILES
O=C1N([C@](CC2)([H])C[C@]2([H])O3)[C@@]3([H])CN(C=C(C([15NH]C([2H])([2H])C(C(F)=CC(F)=C4)=C4F)=O)C5=O)C1=C5O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 83.3 mg/mL (184.13 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2105 mL | 11.0524 mL | 22.1048 mL | 55.2621 mL |
| 5 mM | 0.4421 mL | 2.2105 mL | 4.4210 mL | 11.0524 mL | |
| 10 mM | 0.2210 mL | 1.1052 mL | 2.2105 mL | 5.5262 mL | |
| 15 mM | 0.1474 mL | 0.7368 mL | 1.4737 mL | 3.6841 mL | |
| 20 mM | 0.1105 mL | 0.5526 mL | 1.1052 mL | 2.7631 mL | |
| 25 mM | 0.0884 mL | 0.4421 mL | 0.8842 mL | 2.2105 mL | |
| 30 mM | 0.0737 mL | 0.3684 mL | 0.7368 mL | 1.8421 mL | |
| 40 mM | 0.0553 mL | 0.2763 mL | 0.5526 mL | 1.3816 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4421 mL | 1.1052 mL | |
| 60 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9210 mL | |
| 80 mM | 0.0276 mL | 0.1382 mL | 0.2763 mL | 0.6908 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5526 mL |
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