RO2959 Hydrochloride

SKU: orb1219024

Description

RO2959 hydrochloride is a potent and selective inhibitor of CRAC channel(IC50: 402 nM). It is also a potent inhibitor of human IL-2.

Images & Validation

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Key Properties

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CAS Number	1219927-22-6
MW	463.93
Purity	>98% (HPLC)
Formula	C₂₁H₂₀ClF₂N₅OS
SMILES	CC1=C(CN(CC1)C2=NC=C(S2)C)C3=CN=C(C=N3)NC(=O)C4=C(C=CC=C4F)F.Cl
Target	Calcium Channel
Solubility	DMSO:10 mM

Bioactivity

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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. 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).

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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RO2959 HCl

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Gene Symbol

Calcium Channel

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