RO2959 monohydrochloride

Modify Date: 2024-01-13 09:29:10

RO2959 monohydrochloride Structure
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 monohydrochloride


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].

 Names

Name RO2959 monohydrochloride

 RO2959 monohydrochloride Biological Activity

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

[1]. Gang Chen, et al. Characterization of a Novel CRAC Inhibitor That Potently Blocks Human T Cell Activation and Effector Functions. Mol Immunol. 2013 Jul;54(3-4):355-67.

[2]. Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222.

 Chemical & Physical Properties

Molecular Formula C21H20ClF2N5OS
Molecular Weight 463.93

 Safety Information

Hazard Codes Xi