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Merck

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
MDL number:
NACRES:
NA.28

Product Name

Orai1 Agonist, IA65, ≥95% (HPLC)

form

powder

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)

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.

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