[CAS NO. 1611493-60-7] Bictegravir
PRODUCTS SPECIFICATIONS [1611493-60-7]
DESCRIPTION [1611493-60-7]
Overview
| MDL | MFCD31536971 |
|---|---|
| Molecular Weight | 449.38 |
| Molecular Formula | C21H18F3N3O5 |
| SMILES | O=C1N([C@](CC2)([H])C[C@]2([H])O3)[C@@]3([H])CN(C=C(C(NCC(C(F)=CC(F)=C4)=C4F)=O)C5=O)C1=C5O |
6 Publications Citing Use of MCE
Summary
Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC 50 of 7.5 nM.
IC50 & Target
IC50: 7.5 nM (HIV-1 integrase) [1]
In Vitro
Bictegravir (BIC) inhibits the strand transfer activity with an IC 50 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 IC 50 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 EC 50 s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4 + T lymphocytes and monocyte-derived macrophages, with EC 50 s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04518228 | National Institute of Allergy and Infectious Diseases (NIAID)|International Maternal Pediatric Adolescent AIDS Clinical Trials Group|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|National Institute of Mental Health (NIMH)|Gilead Sciences|ViiV Healthcare|Merck Sharp & Dohme LLC |
HIV Infections|Tuberculosis
|
June 8, 2021 | |
| NCT02400307 | Gilead Sciences |
HIV
|
April 17, 2015 | Phase 1 |
| NCT03711253 | University of Southern California |
Acute HIV Infection
|
October 14, 2019 | Phase 4 |
| NCT05502341 | Gilead Sciences |
HIV-1-infection
|
August 16, 2022 | Phase 2|Phase 3 |
| NCT04054089 | Cristina Mussini|University of Modena and Reggio Emilia |
HIV Infections
|
September 2019 | Phase 4 |
| NCT03499483 | Fenway Community Health |
HIV Prevention
|
January 24, 2019 | Phase 4 |
| NCT04712058 | National Taiwan University Hospital|Far Eastern Memorial Hospital|Mackay Memorial Hospital|Changhua Christian Hospital|Chung Shan Medical University|National Cheng-Kung University Hospital|Chi Mei Medical Hospital|Kaohsiung Medical University Chung-Ho Memorial Hospital|Kaohsiung Municipal Ta-Tung Hospital |
HIV Infections
|
January 20, 2021 | Not Applicable |
| NCT04805944 | Cliniques universitaires Saint-Luc- Université Catholique de Louvain |
HIV Infections
|
March 5, 2021 | |
| NCT02275065 | Gilead Sciences |
HIV-1 Infection
|
October 24, 2014 | Phase 1 |
| NCT04853524 | Janssen Research & Development, LLC |
Healthy
|
May 6, 2021 | Phase 1 |
| NCT04585737 | Charlotte-Paige Rolle, MD|ViiV Healthcare|Orlando Immunology Center |
HIV I Infection
|
September 22, 2020 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 83.3 mg/mL ( 185.37 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2253 mL | 11.1264 mL | 22.2529 mL |
| 5 mM | 0.4451 mL | 2.2253 mL | 4.4506 mL |
| 10 mM | 0.2225 mL | 1.1126 mL | 2.2253 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution
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3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution
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4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.56 mM); Clear solution
Synonyms