Boceprevir
394730-60-0
0.98%
2026-06-28
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName Boceprevir Cat No CEI-1259 Description Boceprevir(EBP-520, SCH503034) is an inhibitor of HCV protease with a Ki value of 14 nM. Product Overview Boceprevir is a potent and selective inhibitor of hepatitis C virus (HCV) protease NS3 with Ki value of 14 nM. HCV is a type of RNA virus and infects about 300 million people worldwide. As a serine protease of HCV, NS3 plays an important role in the replication process of HCV when the virus enters the host cell. NS3 processes the polyprotein translated from the virus RNA genome and promotes the maturation of the virus. NS3 is also found to restore the interferon-sensitive signaling pathway. Due to these features, NS3 is thought to be the appropriate target for the therapy of antivirus. The SAR studies led to the discovery of boceprevir (also named as SCH 503034). Boceprevir has a ketoamide group, it binds NS3 and forms a covalent and reversible adduct with the active site serine. In the cell-based replicon assay using hepatocytes, boceprevir showed improved potency than other derivatives with IC90 value of 350 nM. The selectivity of boceprevir was tested by binding to human neutrophil elastase which had similar structure with NS3. Boceprevir exerted a great selectivity with a HNE/HCV ratio of 2200. It is approximately 15-fold more selective than the corresponding carbamate derivative. In MTS assay, the compound showed no significant cytotoxicity even when its concentration was up to 50 μM. Boceprevir is an orally bioavailable inhibitor of HCV NS3 protease. In rats, oral administration of boceprevir showed AUC value of 1.5 μM•H and bioavailability of 26%. In dogs, boceprevir demonstrated a 30% bioavailability with AUC value of 3.1μM•H at a dose of 3 mg/kg. Boceprevir was also used as a combination therapy with the pegylated interferon (PEG-IFN-α-2B). It was found that the combination showed at least addictive potency compared with each one alone. CAS No 394730-60-0 Molecular Weight 519.68 Purity 0.98 Storage Store at -20°C Synonyms Boceprevir,EBP 520; SCH 503034; EBP-520; EBP520; SCH-503034; SCH503034 Targets HCV protease IC50 14 nM (Ki) Molecular Formula C27H45N5O5 Chemical Name (1R,2S,5S)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-[(2S)-2-(tert-butylcarbamoylamino)-3,3-dimethylbutanoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide Solubility Soluble in DMSO Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Bulk Drug Intermediates(c1112) cas_num 394730-60-0 Basic Info-
Product Name:
Boceprevir
Other Name:3-Azabicyclo[3.1.0]hexane-2-carboxamide,N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-,(1R,2S,5S)-;(1R,2S,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide;Sch 503034;Boceprevir;EBP 520;Victrelis;Boceprevirertet
CAS No.:394730-60-0
Molecular Formula:C27H45N5O5
InChIKeys:InChIKey=LHHCSNFAOIFYRV-DOVBMPENSA-N
Molecular Weight:519.6767
Exact Mass:519.68
EC Number:1592732-453-0
UNII:89BT58KELH
NCI Thesaurus Code:C117292
Color/Form:White to off-white amorphous powder
ATC Code:J05AE|J - Antiinfectives for systemic use
Categories:
Characteristics-
PSA:
150.70000
XLogP3:2.05
Density:1.2±0.1 g/cm3
Refractive Index:1.533
Water Solubility:Slightly soluble in water
Storage Conditions:Boceprevir capsules should be refrigerated at 2-8 °C (36-46 °F) until dispensed. Avoid exposure to excessive heat. For patient use, refrigerated capsules of boceprevir can remain stable until the expiration date printed on the label. Bboceprevir also be stored at room temperature up to 25 °C (77 °F) for 3 months. Keep container tightly closed.
Hazard IdentificationClassification of the substance or mixture
Acute toxicity - Category 4, Oral
Reproductive toxicity, Category 2
GHS label elements, including precautionary statements
Pictogram(s) 
Signal word Warning
Hazard statement(s) H361 Suspected of damaging fertility or the unborn child
Precautionary statement(s) Prevention P264 Wash ... thoroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P203 Obtain, read and follow all safety instructions before use.
P280 Wear protective gloves/protective clothing/eye protection/face protection/hearing protection/...
Response P301+P317 IF SWALLOWED: Get medical help.
P330 Rinse mouth.
P318 IF exposed or concerned, get medical advice.
Storage P405 Store locked up.
Disposal P501 Dispose of contents/container to an appropriate treatment and disposal facility in accordance with applicable laws and regulations, and product characteristics at time of disposal.
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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Country Product Purchase Quantity Date Posted Post an enquiry for this product