SMILES string
O=C(C1=CC=C(NC2=NC(C(F)(F)F)=C(C3=CC=CC=C3)S2)C=C1)O
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
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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