Art. -Nr.: HY-121240

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Brecanavir

(Synonyms: GW640385)

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Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.

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Reinheit: 98.79%
CAS. Nr.: 313682-08-5
Formel: C₃₃H₄₁N₃O₁₀S₂
Molecular Weight:703.82

Speicherung:

-20°C, protect from light, stored under nitrogen

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

Brecanavir Chemical Structure

CAS. Nr.: 313682-08-5

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.

Cellular Effect

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]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 313682-08-5
Appearance Solid
Molecular Weight 703.82
Formel C₃₃H₄₁N₃O₁₀S₂
Color White to off-white
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
Synonyms

GW640385
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light, stored under nitrogen

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

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4208 mL

7.1041 mL

14.2082 mL

5 mM

0.2842 mL

1.4208 mL

2.8416 mL

10 mM

0.1421 mL

0.7104 mL

1.4208 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Brecanavir

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Brecanavir Related Classifications

HY-121240 Related Classifications