SML4116

Orai1 Agonist, IA65

≥95% (HPLC)

• Synonyme(s) : 4-((5-Phenyl-4-(trifluoromethyl)thiazol-2-yl)amino)benzoic acid, 4-[[5-Phenyl-4-(trifluoromethyl)-2-thiazolyl]amino]benzoic acid, IA65
• Formule empirique (notation de Hill) : C₁₇H₁₁F₃N₂O₂S
• Numéro CAS: 255833-41-1
• Poids moléculaire : 364.34
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: 2-8°C

Description

Actions biochimiques/physiologiques

Selective Orai1 and SOCE (store-operated Ca2+ entry) potentiator that marginally affects Orai2 and Orai3.
Orai1 Agonist IA65 is a selective Orai1 and SOCE (store-operated Ca2+ entry) potentiator that preferentially occupies Oari1 N-terminal domain binding pocket and significantly enhances Orai1-mediated Ca2+-influx and concurrently potentiates Orai1 Ca2+-dependent inactivation (CDI) with an EC50 of 1.9 uM. IA65 mildly potentiates ORAI3-mediated ICRAC with a slight inhibition of ICRAC mediated by ORAI2. Increases Orai1 activity in VSMCs and skeletal muscle fibers in a concentration-dependent manner. IA-65 is shown to be inactive against TRPV1, TRPM8, or CaV2.2 and nontoxic up to 100 uM.