RO2959 Hydrochloride

Product Name: RO2959 Hydrochloride
CAS No.: 1219927-22-6
Chemical Name: RO2959 Hydrochloride
Synonyms: SYN5226;RO2959 HCl;RO2959 Hydrochloride;RO2959 Hydrochloride, 10 mM in DMSO;IP3,SOCE,Ca2+ release-activated Ca2+ channels,RO2959 Hydrochloride,Interleukin Related,inhibit,IL-2,Stim1,RO-2959 Hydrochloride,CRAC Channel,anti-proliferation,RO 2959,Calcium release-activated channels,T-cell,RO-2959,Orai1,heart,RO2959,Inhibitor,failure
CBNumber: CB23067576
Molecular Formula: C21H20ClF2N5OS
Formula Weight: 463.93
MOL File: 1219927-22-6.mol

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RO2959 Hydrochloride Property

storage temp.: Store at -20°C
form: Solid
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0063986
Product name: RO2959hydrochloride
Packaging: 5mg
Price: $350
Updated: 2021/12/16

AK Scientific

Product number: SYN5226
Product name: RO2959Hydrochloride
Packaging: 100mg
Price: $2635.25
Updated: 2021/12/16

DC Chemicals

Product number: DC33579
Product name: RO2959Hydrochloride
Packaging: 100mg
Price: $750
Updated: 2021/12/16

DC Chemicals

Product number: DC33579
Product name: RO2959Hydrochloride
Packaging: 1g
Price: $2600
Updated: 2021/12/16

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RO2959 Hydrochloride Chemical Properties,Usage,Production

Uses

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].

Biological Activity

RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with IC50 of 402 nM. It is a potent blocker of Orai1/Stim1 channel-mediated calcium storage entry (SOCE) with IC50 of 25 nM. It is also a potent inhibitor of human IL-2 production, effectively blocking T cell receptor-triggered gene expression and T cell functional pathways.

in vitro

RO2959 hydrochloride inhibits Orai1 and Orai3 with IC ₅₀ values of 25 nM and 530 nM, respectively. It blocks store operated calcium entry (SOCE) in activated CD4+T lymphocytes with an IC < sub> 50 value of 265 nM.
It 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 ).

target

CRAC channel

402 nM (IC ₅₀ )

Orai1/Stim1 channels

25 nM (IC ₅₀ )

IL-2

IC 50

CRAC channel: 402 nM (IC₅₀); Orai1/Stim1 channels: 25 nM (IC₅₀); IL-2

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. DOI:10.1016/j.molimm.2012.12.011
[2] Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222. DOI:10.3389/fphar.2017.00222

RO2959 Hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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RO2959 Hydrochloride Suppliers

China 37 United Kingdom 1 United States 5 Global 43

Shanghai Lollane Biological Technology Co.,Ltd.

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Pharmacodia (Beijing) Co.,Ltd

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Shanghai Haozhixiang Biotechnology Co., Ltd

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Shanghai EFE Biological Technology Co., Ltd.

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ShangHai Biochempartner Co.,Ltd

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Lynnchem

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Novachemistry

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Shanghai Hongye Biotechnology Co. Ltd

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TargetMol Chemicals Inc.

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RO2959 Hydrochloride

RO2959 HCl

IP3,SOCE,Ca2+ release-activated Ca2+ channels,RO2959 Hydrochloride,Interleukin Related,inhibit,IL-2,Stim1,RO-2959 Hydrochloride,CRAC Channel,anti-proliferation,RO 2959,Calcium release-activated channels,T-cell,RO-2959,Orai1,heart,RO2959,Inhibitor,failure

SYN5226

RO2959 Hydrochloride, 10 mM in DMSO

1219927-22-6