5.30647

Orai1/CRAC Blocker, Cpd5J-4

• Synonym(s): Orai1/CRAC Blocker, Cpd5J-4, Orai1 Inhibitor, CRAC Inhibitor, Ca ²⁺ release-activated Ca ²⁺ (CRAC) channel blocker
• Empirical Formula (Hill Notation): C₁₆H₁₂N₂O₃S
• CAS Number: 827001-82-1
• Molecular Weight: 312.34
• MDL number: MFCD05832424
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• storage temp.: −20°C

Description

General description

A non-toxic thiourea derivative that acts as a blocker of Orai1, the pore subunit of Ca2+-release-activated Ca2+ (CRAC) in T cells. Exhibits a strong blocking effect on store-operated Ca2+ entry in HeLa-O+S cells and in Th17 cells. Preferentially reduces Th17 differentiation and ameliorates Th17-mediated autoimmune disease. Blocks the infiltration of T cells into the CNS and reduces the number of IL-17 producing cells. Also shown to reduce the expression of retinoic acid receptor-related orphan receptors a (RORa) and RORgt. Reduces the symptoms and delays the onset of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoproteins 35-55 (MOG35-55) immunized mice (2 mg/kg, i.p.).

A non-toxic thiourea derivative that acts as a blocker of Orai1, the pore subunit of Ca²⁺-release-activated Ca²⁺ (CRAC) in T cells. Exhibits a strong blocking effect on store-operated Ca²⁺ entry in HeLa-O+S cells and in Th17 cells. Preferentially reduces Th17 differentiation and ameliorates Th17-mediated autoimmune disease. Blocks the infiltration of T cells into the CNS and reduces the number of IL-17 producing cells. Also shown to reduce the expression of retinoic acid receptor-related orphan receptors a (RORa) and RORgt. Reduces the symptoms and delays the onset of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoproteins 35-55 (MOG35-55) immunized mice (2 mg/kg, i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Primary Target
Orail1

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Kim, K., et al. 2014. J Immunol.192, 110.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

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