ORAI1/CRAC BLOCKER CPD5J-4 (C15-1305-025)

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

Molecular Weight: 312.34. Empirical Formula: C₁₆H₁₂N₂O₃S. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.