RO2959 monohydrochloride structure
|
Common Name | RO2959 monohydrochloride | ||
|---|---|---|---|---|
| CAS Number | 2309172-44-7 | Molecular Weight | 463.93 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H20ClF2N5OS | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of RO2959 monohydrochlorideRO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride 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 | RO2959 monohydrochloride |
|---|
| Description | RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride 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]. |
|---|---|
| Related Catalog | |
| Target |
IL-2 CRAC channel:402 nM (IC50) Orai1/Stim1 channels:25 nM (IC50) |
| 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 | C21H20ClF2N5OS |
|---|---|
| Molecular Weight | 463.93 |
| Hazard Codes | Xi |
|---|