SML1925

Bepristat 2a hydrochloride

≥95% (HPLC)

• Synonym(s): 6-Bromo-2-[[[2-(diethylamino)ethyl]amino]methyl]-5-hydroxy-1-phenyl-1H-indole-3-carboxylic acid ethyl ester hydrochloride
• Empirical Formula (Hill Notation): C₂₄H₃₀BrN₃O₃ · xHCl
• CAS Number: 2140803-90-1
• Molecular Weight: 488.42 (free base basis)
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: H₂O: 10 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CCN(CC)CCNCC1=C(C(OCC)=O)C2=CC(O)=C(Br)C=C2N1C3=CC=CC=C3.[H]Cl

Description

Biochem/physiol Actions

Bepristat 2a is a selective reversible inhibitor of protein disulfide isomerase (PDI), an enzyme in the endoplasmic reticulum that catalyzes disulfide bond breakage and reformation to catalyze protein folding. Unlike most PDI inhibitors, Bepristat 2a binds at the substrate-binding site, rather than the catalytic site. Bepristat 2a blocked PDI activity with an IC₅₀ value of 1200 nM, while enhancing catalytic activity of remote PDI domains. PDI is up-regulated in several cancers, has been implicated in neurodegenerative processes, and plays an important role in thrombus formation. Bepristat 2a potently inhibited platelet aggregation and thrombus formation in vivo.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable