Orai1/CRAC Blocker, Cpd5J-4

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.

Primary Target
Orail1

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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

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