The Ca2+ release-activated Ca2+ (CRAC) channel is a highly Ca2+-selective store-operated channel expressed in T cells, mast cells, and various other tissues. CRAC channels regulate critical cellular processes such as gene expression, motility, and the secretion of inflammatory mediators. The identification of Orai1, a key subunit of the CRAC channel pore, and STIM1, the endoplasmic reticulum (ER) Ca2+ sensor, have provided the tools to illuminate the mechanisms of regulation and the pore properties of CRAC channels. Opening of CRAC channels enables the refilling of ER Ca2+ stores and sustains long-lasting Ca2+ oscillations and plateau signals, critical for the proliferation of T cells and production of cytokines following antigenic stimulation.


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CRAC intermediate 1

CRAC intermediate 1 is a key intermediate in the chemical synthesis of a series of CRAC channel inhibitors, detailed information can be found in Patent WO 2010122089 A1, intermediate 9.

  • CAS Number: 1249343-86-9
  • MF: C10H7F2N3O
  • MW: 223.17900
  • Catalog: CRAC Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5J-4

5J-4 is a potent CRAC inhibitor. 5J-4 decreases the numbers of infiltrated mononuclear cell into the CNS, and significantly decreases the population of infiltrated CD4+ population. 5J-4 reduces the symptoms and delayed the onset of EAE (experimental autoimmune encephalomyelitis) in mouse model of inflammation[1].

  • CAS Number: 827001-82-1
  • MF: C16H12N2O3S
  • MW: 312.34
  • Catalog: CRAC Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GSK-5498A

GSK-5498A is a selective small molecule blocker of CRAC channel(IC50=1 uM); inhibit mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.IC50 value: 1 uM [1]Target: CARC channel blocker GSK-5498A completely inhibited calcium influx through CRAC channels. This led to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations. Mast cells from guinea-pig and mouse preparations were not inhibited by GSK-5498A.

  • CAS Number: 1253186-49-0
  • MF: C18H11F6N3O
  • MW: 399.290
  • Catalog: CRAC Channel
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 403.3±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 197.7±28.7 °C

GSK-5503A

Novel selective CRAC channel blocker

  • CAS Number: 1253186-46-7
  • MF: C23H17F2N3O2
  • MW: 405.40
  • Catalog: CRAC Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CM-4620

CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

  • CAS Number: 1713240-67-5
  • MF: C19H11ClF3N3O3
  • MW: 421.757
  • Catalog: CRAC Channel
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 444.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.5±28.7 °C

4-(3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl)phenylamine

CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.

  • CAS Number: 123066-64-8
  • MF: C11H7F6N3
  • MW: 295.184
  • Catalog: CRAC Channel
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 298.4±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 134.3±27.3 °C

Synta66

Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.

  • CAS Number: 835904-51-3
  • MF: C20H17FN2O3
  • MW: 352.359
  • Catalog: CRAC Channel
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 422.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 209.3±28.7 °C

YM-58483

YM-58483 is the first selective and potent inhibitor of CRAC channels and subsequent Ca2+ signals.

  • CAS Number: 223499-30-7
  • MF: C15H9F6N5OS
  • MW: 421.320
  • Catalog: CRAC Channel
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RO2959 hydrochloride

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].

  • CAS Number: 1219927-22-6
  • MF: C21H19F2N5OS.xHCl
  • MW: 463.931
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

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].

  • CAS Number: 2309172-44-7
  • MF: C21H20ClF2N5OS
  • MW: 463.93
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

piCRAC-1

piCRAC-1 is a potent, photoinducible Ca2+ release-activated Ca2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage[1].

  • CAS Number: 2418049-54-2
  • MF: C17H10F6N4
  • MW: 384.28
  • Catalog: CRAC Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SOCE inhibitor 1

SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC50 of 4.4 μM.

  • CAS Number: 2169316-15-6
  • MF: C25H22F3N5O4
  • MW: 513.47
  • Catalog: CRAC Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A