Brecanavir
Based on 1 Customer Validation
Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.79%
- CAS 番号: 313682-08-5
- 分子式: C33H41N3O10S2
- 分子量:703.82
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
>90000 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human HeLa cells by HeLa-CD4 MAGI assay
Antiviral activity against HIV1 HXB2 in human HeLa cells by HeLa-CD4 MAGI assay
|
[PMID: 17620375] |
| MDCK-II | IC50 |
24.1 μM
Compound: BRV
|
Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells
Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells
|
[PMID: 17664327] |
| MT2 | IC50 |
0.0002 μM
Compound: BCV, brecanavir
|
Antiviral activity against HIV1 LAI in MT2 cells
Antiviral activity against HIV1 LAI in MT2 cells
|
[PMID: 17635930] |
| MT2 | IC50 |
0.2 nM
Compound: BCV, brecanavir
|
Antiviral activity against HIV1 LAI in MT2 cells
Antiviral activity against HIV1 LAI in MT2 cells
|
[PMID: 17635930] |
| MT4 | IC50 |
0.22 nM
Compound: 27
|
Antiviral activity against HIV1 I54V in MT4 cells
Antiviral activity against HIV1 I54V in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
0.45 nM
Compound: 27
|
Antiviral activity against nelfinavir resistant HIV1 14330 in MT4 cells
Antiviral activity against nelfinavir resistant HIV1 14330 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
0.46 nM
Compound: 27
|
Antiviral activity against indinavir resistant HIV1 30813 in MT4 cells
Antiviral activity against indinavir resistant HIV1 30813 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
0.7 nM
Compound: 27
|
Antiviral activity against HIV1 HXB2 in MT4 cells
Antiviral activity against HIV1 HXB2 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
0.77 nM
Compound: 27
|
Antiviral activity against multi PI resistant HIV1 EP14 in MT4 cells
Antiviral activity against multi PI resistant HIV1 EP14 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
1.1 nM
Compound: 27
|
Antiviral activity against HIV1 EP13 in MT4 cells
Antiviral activity against HIV1 EP13 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
1.6 nM
Compound: 27
|
Antiviral activity against HIV1 I50V in MT4 cells
Antiviral activity against HIV1 I50V in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
1.7 nM
Compound: 27
|
Antiviral activity against multi PI resistant HIV1 31246 in MT4 cells
Antiviral activity against multi PI resistant HIV1 31246 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
4.8 nM
Compound: 27
|
Antiviral activity against HIV D545701 in MT4 cells
Antiviral activity against HIV D545701 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
5.4 nM
Compound: 27
|
Antiviral activity against triple multi PI resistant HIV1 in MT4 cells
Antiviral activity against triple multi PI resistant HIV1 in MT4 cells
|
[PMID: 16458505] |
| MT4 | IC50 |
8.2 nM
Compound: 27
|
Antiviral activity against amprenavir resistant HIV1 468 in MT4 cells
Antiviral activity against amprenavir resistant HIV1 468 in MT4 cells
|
[PMID: 16458505] |
| MT4 | EC50 |
0.44 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect by MTS assay
Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
0.53 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
0.7 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
1.1 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 40% fetal bovine serum by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
1.4 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 10% human serum by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
2.2 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 20% human serum by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
2.6 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 30% human serum by MTS assay
|
[PMID: 17620375] |
| MT4 | EC50 |
3.8 nM
Compound: BCV, GW-640385
|
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay
Antiviral activity against HIV1 HXB2 in human MT4 cells assessed as inhibition of viral-induced viral cytopathic effect in presence of 10% fetal bovine serum and 40% human serum by MTS assay
|
[PMID: 17620375] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 313682-08-5
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性状 Solid
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分子量 703.82
-
分子式 C33H41N3O10S2
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Color White to off-white
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SMILES
CC1=NC(COC2=CC=C(C[C@H](NC(O[C@H]3CO[C@@H]4[C@H]3CCO4)=O)[C@H](O)CN(S(=O)(C5=CC=C6C(OCO6)=C5)=O)CC(C)C)C=C2)=CS1
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別名
GW640385
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : 17.6 mg/mL (25.01 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, stored under nitrogen). 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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ford SL, Reddy YS, Anderson MT, et al. Single-dose safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus protease inhibitor. Antimicrob Agents Chemother. 2006;50(6):2201-2206. [Content Brief]
[2]. Reddy YS, Ford SL, Anderson MT, Murray SC, Ng-Cashin J, Johnson MA. Safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus type 1 protease inhibitor, following repeat administration with and without ritonavir in healthy adult subj [Content Brief]
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, stored under nitrogen). 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 | 1.4208 mL | 7.1041 mL | 14.2082 mL | 35.5204 mL |
| 5 mM | 0.2842 mL | 1.4208 mL | 2.8416 mL | 7.1041 mL | |
| 10 mM | 0.1421 mL | 0.7104 mL | 1.4208 mL | 3.5520 mL | |
| 15 mM | 0.0947 mL | 0.4736 mL | 0.9472 mL | 2.3680 mL | |
| 20 mM | 0.0710 mL | 0.3552 mL | 0.7104 mL | 1.7760 mL | |
| 25 mM | 0.0568 mL | 0.2842 mL | 0.5683 mL | 1.4208 mL |