VRT-043198 - 10mM in DMSO , CAS No.244133-31-1

CAS: 244133-31-1 Cat. No.: V655393 Formula: C₂₂H₂₉ClN₄O₆ Peso molecolare: 480.9 PubChem CID: 11443029

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits K i values of 0.8 nM and 0.6 nM for ICE/caspase-1 and caspase-4, respectively

In Vitro

VRT-043198 exhibits 100- to 10,000-fold selectivity against other caspase-3 and -6 to -9. VRT043198 inhibits the release of interleukin (IL)-1β and IL-18, but it has little effect on the release of several other cytokines, including IL-1α, tumor necrosis factor-, IL-6 and IL-8. VRT-043198 inhibited IL-1β release from both PBMCs (n = 8) and whole blood (n = 4) with IC 50 values of 0.67±0.55 and 1.9±0.80 nM, respectively. VRT-043198 lacks potent antiapoptotic activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

VX-765 is converted rapidly to VRT-043198 under the action of plasma and liver esterases and also much more slowly in aqueous solution . VX765 reduces disease severity and the expression of inflammatory mediators in models of rheumatoid arthritis and skin inflammation . VX765 (25, 50, 100, or 200 mg/kg) inhibits lipopolysaccharide-induced cytokine secretion . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naïve male CD-1 mice . Dosage: 25-200 mg/kg. Administration: Oral gavage 1 h before i.v. injection of 2 mg/kg E. coli LPS (strain 0111:B4). Result: Reduced serum IL-1β levels.

IC50& Target:Caspase-1 0.8 nM (Ki) Caspase-4 0.6 nM (Ki)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

VRT-043198, the agent metabolite of VX-765 (Belnacasan), is a potent, selective and blood-brain barrier permeable inhibitor of interleukin-converting enzyme/caspase-1 subfamily caspases. VRT-043198 exhibits K i values of 0.8 nM and 0.6 nM for ICE/caspase-

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Nomi e identificatori

• Isomeri SMILES: CC(C)(C)[C@@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C=O)NC(=O)C2=CC(=C(C=C2)N)Cl
• CAS alternativo: 244133-31-1
• PubChem CID: 11443029
• Termini MeSH: (S)-1-((S)-2-1((-(4-amino-3-chloro-phenyl)-methanoyl)-amino)-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide;(S)-3-((1-((S)-1-((S)-2-((1-(4-amino-3-chlorophenyl)methanoyl)amino)-3,3-dimethyl-butano
• Peso molecolare: 480.9

Obiettivi associati (umani)

CASP1 Tchem Caspase-1 (0 Activities)

Discover Target: CASP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CASP4 Tchem Caspase-4 (0 Activities)

Discover Target: CASP4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 244133-31-1, the molecular formula is C22H29ClN4O6, and the molecular weight is 480.9 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.