2. Others
  3. Isotope-Labeled Compounds
  4. Bictegravir-15N,d2

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.

Bictegravir-<sup>15</sup>N,d<sub>2</sub> Chemical Structure

Bictegravir-15N,d2 Chemical Structure

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Based on 1 publication(s) in Google Scholar

Other Forms of Bictegravir-15N,d2:

Bictegravir-15N,d2 Related Antibodies

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Description

Bictegravir-15N,d2 (GS-9883-15N,d2) is the 15N and deuterium labeled Bictegravir (HY-17605)[1]. Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM[2].

IC50 & Target

IC50: 7.5 nM (HIV-1 integrase)[1]
In Vitro

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.

Bictegravir-15N,d2 Related Antibodies
Molecular Weight

452.39

Formula

C21H16D2F3N215NO5
Unlabeled CAS

1611493-60-7
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2105 mL 11.0524 mL 22.1048 mL
5 mM 0.4421 mL 2.2105 mL 4.4210 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 96.09%

SDS (557 KB)

COA (250 KB)

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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Bictegravir-15N,d2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bictegravir-15N,d2Isotope-Labeled CompoundsInhibitorinhibitorinhibit

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