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 Ca release-activated Ca (CRAC) channel is a

2、 highly Ca-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 channel por

3、e, and STIM1, the endoplasmic reticulum(ER) Ca 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 concentration, and in turn, areresponsible for re

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

5、RAC 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 https:/www.MedChemE

6、/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 https:/www.MedC

7、hemE/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-intermediate-1.html HY

8、PERLINK 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 intermediate 1 is a key in

9、termediate 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, 5 mg, 10 mg, 50

10、 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-intermediate-2.

11、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 selective small mol

12、ecule blocker ofCARC (IC , 1 M); inhibits mediator release frommast 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 Development Repo

13、rtedSize: 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 inhibitor with an IC o

14、f 1.7 M.MRS1845 is an ORAI1 inhibitor.piCRAC-1 is a potent, photoinducible Carelease-activated Ca (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%Clinical Data: No Development

15、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 HYPERLINK https:/www.MedChemE/

16、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 inhibitor with an IC of 40

17、2 nM.RO2959 hydrochloride is a potent blocker of storeoperated calcium entry (SOCE) mediated byOrai1/Stim1 channels with an IC of 25 nM.RO2959 monohydrochloride is a potent and selectiveCRAC channel inhibitor with an IC of 402 nM.RO2959 monohydrochloride is a potent blocker ofstore operated calcium

18、entry (SOCE) mediated byOrai1/Stim1 channels with an IC of 25 nM.Purity: 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.html SKF-96365 HYPERLINK https

19、:/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_inhibitor_1.html HYPERLINK https

20、:/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 entry (SOCE)inhibitor. SKF-963

21、65 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.Purity: 99.51%Clinical Data: No Development ReportedS

22、ize: 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-111325 HYPERLINK https:/www.MedChemE

23、/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 https:/www.MedChemE/Tanshinone-IIA-s

24、ulfonate-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 IIAsulfonate; Tanshinone IIA sodium sulfon

25、ate) 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 Ca entry (SOCE), and is used totreat cardiovascular disord