SML4116
Orai1 Agonist, IA65
≥95% (HPLC)
Synonym(s):
4-((5-Phenyl-4-(trifluoromethyl)thiazol-2-yl)amino)benzoic acid, 4-[[5-Phenyl-4-(trifluoromethyl)-2-thiazolyl]amino]benzoic acid, IA65
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About This Item
Empirical Formula (Hill Notation):
C17H11F3N2O2S
CAS Number:
Molecular Weight:
364.34
UNSPSC Code:
12352200
Quality Level
Assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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.
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.
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