DC Chemicals Limited
China
Product Name: RO2959 monohydrochloride
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

2309172-44-7

2309172-44-7 structure

Name: RO2959 monohydrochloride
Chemical Name: RO2959 monohydrochloride
CAS Number: 2309172-44-7
Molecular Formula: C₂₁H₂₀ClF₂N₅OS
Molecular Weight: 463.93
Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
Create Date: 2020-10-26 11:20:24
Modify Date: 2024-01-13 09:29:10
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].

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	Research Areas >> Cardiovascular Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> CRAC Channel Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
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.

Molecular Formula	C₂₁H₂₀ClF₂N₅OS
Molecular Weight	463.93

Hazard Codes	Xi

2309172-44-7	1219927-22-6
100694-13-1	923288-90-8
593-81-7	59461-30-2
19341-56-1	5103-96-8
127881-54-3	58296-58-5