1、 HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html CRAC HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html ChannelCalcium release-activated channels; Ca2+ release-activated Ca2+ channelsThe Ca2+ release-activated Ca2+ (CRAC) channel

2、is a highly Ca2+-selective store-operated channel expressed in T cells, mast cells, andvarious other tissues. CRAC channels regulate critical cellular processes such as gene expression, motility, and the secretion ofinflammatory mediators. The identification of Orai1, a key subunit of the CRAC chann

3、el 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.STIM1 proteins span through the membrane of the ER, are competent in sensing luminal Ca 2+ concentration, and in turn, arerespons

4、ible for relaying the signal of Ca2+ store-depletion to pore-forming Orai1 proteins in the plasma membrane. A directinteraction of STIM1 and Orai1 allows for the re-entry of Ca2+ from the extracellular space. CRAC channels are critical forlymphocyte function and immune responses. A driving force in

5、the quest for CRAC channel drugs has been theimmunocompromised phenotype displayed by humans and mice with null or loss-of-function mutations in STIM1 or Orai1,suggesting that CRAC channel inhibitors could be useful therapeutics for autoimmune or inflammatory conditions.www.MedChemE 1 HYPERLINK http

6、s:/www.MedChemE/Targets/CRAC Channel.html CRAC HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html Channel HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html HYPERLINK https:/www.MedChemE/Targets/CRAC Channel.html Inhibitors HYPERLINK

7、https:/www.MedChemE/5j-4.html 5J-4 HYPERLINK https:/www.MedChemE/5j-4.html HYPERLINK https:/www.MedChemE/CRAC-intermediate-1.html CRAC HYPERLINK https:/www.MedChemE/CRAC-intermediate-1.html HYPERLINK https:/www.MedChemE/CRAC-intermediate-1.html intermediate HYPERLINK https:/www.MedChemE/CRAC-interme

8、diate-1.html HYPERLINK https:/www.MedChemE/CRAC-intermediate-1.html 1Cat. No.: HY-110216 Cat. No.: HY-205875J-4 is a potent CRAC inhibitor. 5J-4 decreasesthe numbers of infiltrated mononuclear cell intothe CNS, and significantly decreases thepopulation of infiltrated CD4+ population.CRAC intermediat

9、e 1 is a key intermediate in thechemical synthesis of a series of CRAC channelinhibitors, detailed information can be found inPatent WO 2010122089 A1, intermediate 9.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL,

10、5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CRAC-intermediate-2.html CRAC HYPERLINK https:/www.MedChemE/CRAC-intermediate-2.html HYPERLINK https:/www.MedChemE/CRAC-intermediate-2.html intermediate HYPERLINK https:/www.MedChemE/CRAC-intermediate-2.html HYPERLINK https:/www.MedChemE/CRAC-

11、intermediate-2.html 2 HYPERLINK https:/www.MedChemE/CRAC-intermediate-2.html HYPERLINK https:/www.MedChemE/GSK-5498A.html GSK-5498ACat. No.: HY-20588 Cat. No.: HY-12521CRAC intermediate 2 is a intermediate compound forCRAC inhibitor synthesis, extracted from patent WO2013059666A1.GSK-5498A is a sele

12、ctive small molecule blocker ofCARC (IC , 1 M); inhibits mediator release from50mast cells, and pro-inflammatory cytokine releasefrom T-cells in a variety of species.Purity: 99.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.14%Clinical Data: No

13、 Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/mrs1845.html MRS1845 HYPERLINK https:/www.MedChemE/mrs1845.html HYPERLINK https:/www.MedChemE/picrac-1.html piCRAC-1Cat. No.: HY-103310 Cat. No.: HY-147005MRS1845 is a selective store-operated calcium(SOC) channel inhib

14、itor with an IC of 1.7 M.50MRS1845 is an ORAI1 inhibitor.piCRAC-1 is a potent, photoinducible Ca2+release-activated Ca2+ (CRAC) channel inhibitor.piCRAC-1 alleviates thrombocytopenia andhemorrhage.Purity: 99.27%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinica

15、l Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ro2959-hydrochloride.html RO2959 HYPERLINK https:/www.MedChemE/ro2959-hydrochloride.html HYPERLINK https:/www.MedChemE/ro2959-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/ro2959-hydrochloride.html HYPERLI

16、NK https:/www.MedChemE/ro2959-monohydrochloride.html RO2959 HYPERLINK https:/www.MedChemE/ro2959-monohydrochloride.html HYPERLINK https:/www.MedChemE/ro2959-monohydrochloride.html monohydrochlorideCat. No.: HY-113618A Cat. No.: HY-113618BRO2959 hydrochloride is a potent and selectiveCRAC channel inh

17、ibitor with an IC of 402 nM.50RO2959 hydrochloride is a potent blocker of storeoperated calcium entry (SOCE) mediated byOrai1/Stim1 channels with an IC of 25 nM.50RO2959 monohydrochloride is a potent and selectiveCRAC channel inhibitor with an IC of 402 nM.50RO2959 monohydrochloride is a potent bloc

18、ker ofstore operated calcium entry (SOCE) mediated byOrai1/Stim1 channels with an IC of 25 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.02%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/SKF-96365-hydrochloride

19、.html SKF-96365 HYPERLINK https:/www.MedChemE/SKF-96365-hydrochloride.html HYPERLINK https:/www.MedChemE/SKF-96365-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/SKF-96365-hydrochloride.html HYPERLINK https:/www.MedChemE/SOCE_inhibitor_1.html SOCE HYPERLINK https:/www.MedChemE/SOCE_i

20、nhibitor_1.html HYPERLINK https:/www.MedChemE/SOCE_inhibitor_1.html inhibitor HYPERLINK https:/www.MedChemE/SOCE_inhibitor_1.html HYPERLINK https:/www.MedChemE/SOCE_inhibitor_1.html 1Cat. No.: HY-100001 Cat. No.: HY-112913SKF-96365 hydrochloride is a potent TRP channelblocker and a store-operated Ca

21、2+ entry (SOCE)inhibitor. SKF-96365 hydrochloride significantlyinhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3current, and significantly prolongs the QTcinterval in isolated guinea pig hearts.SOCE inhibitor 1 is a store-operated calciumentry (SOCE) inhibitor with an IC of 4.4 M.50Purity: 99.51%Clin

22、ical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Synta66.html Synta66Cat. No.: HY-1

23、11325 HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html Tanshinone HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html IIA HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html HYPERLINK h

24、ttps:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html sulfonate HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html sodium HYPERLINK https:/www.MedChemE/Tanshinone-IIA-sulfonate-sodium.html (Sodium Tanshinone IIAsulf

25、onate; Tanshinone IIA sodium sulfonate) Cat. No.: HY-N1370Synta66 is an inhibitor of store-operated calciumentry channel Orai, which forms the pore of theCRAC channel, and used for the research ofneurological disease.Tanshinone IIA sulfonate (sodium) is a derivativeof tanshinone IIA, which acts as an inhibitor ofstore-operated Ca2+ entry (SOCE), and is used totreat cardiovascular disorder