RO2959 hydrochloride structure
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Common Name | RO2959 hydrochloride | ||
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| CAS Number | 1219927-22-6 | Molecular Weight | 463.931 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H19F2N5OS.xHCl | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RO2959 hydrochlorideRO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways[1][2]. |
| Name | 2,6-Difluoro-N-{5-[4-methyl-1-(5-methyl-1,3-thiazol-2-yl)-1,2,5,6-tetrahydro-3-pyridinyl]-2-pyrazinyl}benzamide hydrochloride (1:1) |
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| Synonym | More Synonyms |
| Description | RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways[1][2]. |
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| Related Catalog | |
| Target |
IC50: 402 nM (CRAC channel); 25 nM (Orai1/Stim1 channels)[1] IL-2 production[1] |
| In Vitro | RO2959 inhibits Orai1 and Orai3 with IC50 values of 25 nM and 530 nM, respectively. RO2959 blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC50 value of 265 nM[1]. RO2959 is a potent SOCE inhibitor that blocks an IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells stably expressing human Orai1 and Stim1, as well as SOCE in human primary CD4+ T cells triggered by either T cell receptor (TCR) stimulation or thapsigargin treatment. RO2959 completely inhibits cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction)[1]. |
| References |
| Molecular Formula | C21H19F2N5OS.xHCl |
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| Molecular Weight | 463.931 |
| Exact Mass | 463.104523 |
| InChIKey | GMLSDODALBRLPE-UHFFFAOYSA-N |
| SMILES | CC1=C(c2cnc(NC(=O)c3c(F)cccc3F)cn2)CN(c2ncc(C)s2)CC1.Cl |
| Hazard Codes | Xi |
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| Benzamide, 2,6-difluoro-N-[5-[1,2,5,6-tetrahydro-4-methyl-1-(5-methyl-2-thiazolyl)-3-pyridinyl]-2-pyrazinyl]-, hydrochloride (1:1) |
| 2,6-Difluoro-N-{5-[4-methyl-1-(5-methyl-1,3-thiazol-2-yl)-1,2,5,6-tetrahydro-3-pyridinyl]-2-pyrazinyl}benzamide hydrochloride (1:1) |