P2X-Receptor-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html P2X HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html ReceptorP2XRsP2X receptors are a family of seven (P2X1R-P2X7R) cation permeable ligand-gated ion channels (LGICs) that open in

2、response tobinding by the extracellular ligand, adenosine 5-triphosphate (ATP). P2X receptors have a high permeability to Ca2+, Na+, and K+and are expressed widely throughout the nervous, immune, cardiovascular, skeletal, gastrointestinal, respiratory, and endocrinesystems.P2X receptors are widely e

3、xpressed in excitatory and non-excitatory cells, such as neuron, glia, platelet, epithelia and macrophage,and participate in many important physiological and pathological processes, including synaptic transmission, pain perception,inflammation, cardiovascular modulation, immunomodulation and tumorig

4、enesis.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html P2X HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X

5、 Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html Antagonists HYPERLINK https:/www.MedChe

6、mE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html & HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html HYPERLINK https:/www.MedChemE/Targets/P2X Receptor.html Modulators HYPERLINK https:/www.MedChemE/e-z-sivopixant.html (E/Z)-Sivopixant(E/Z)-S-600918) Cat. No.

7、: HY-137451A HYPERLINK https:/www.MedChemE/5-bdbd.html 5-BDBDCat. No.: HY-101911(E/Z)-Sivopixant (E/Z)-S-600918) is a potentP2X3 receptor antagonist with an IC of 4 nM.50(E/Z)-Sivopixant can be used for respiratorydiseases research.5-BDBD, a potent and selective P2X4 receptorantagonist, inhibits rP2

8、X4R-mediated currents,with an IC of 0.75 M. 5-BDBD completely blocks50the basal and acute hyperalgesia induced bynitroglycerin (NTG).Purity: 98.64%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 96.76%Clinical Data: No Development ReportedSize: 5 mg,

9、10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/8-bromo-atp.html 8-Bromo-ATP(8-Bromoadenosine 5-triphosphate; 8-Br-ATP) Cat. No.: HY-134262 HYPERLINK https:/www.MedChemE/a-438079.html A HYPERLINK https:/www.MedChemE/a-438079.html HYPERLINK https:/www.MedChemE/a-438079.html 438079Cat. No.: HY-15488

10、8-Bromo-ATP (8-Bromoadenosine 5-triphosphate), anATP analogue, is a purinergic P2X receptoragonist. 8-Bromo-ATP shows cytotoxic to multiplemyeloma cells with an IC of 23.1 M.50A 438079 is a potent, and selective P2X7receptor antagonist with pIC of506.9.Purity: 98%Clinical Data: No Development Report

11、edSize: 1 mgPurity: 99.74%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/A-438079-hydrochloride.html A HYPERLINK https:/www.MedChemE/A-438079-hydrochloride.html HYPERLINK https:/www.MedChemE/A-438079-hydrochloride.html 438079 HYPERLINK http

12、s:/www.MedChemE/A-438079-hydrochloride.html HYPERLINK https:/www.MedChemE/A-438079-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/A-438079-hydrochloride.html HYPERLINK https:/www.MedChemE/a-839977.html A HYPERLINK https:/www.MedChemE/a-839977.html HYPERLINK https:/www.MedChemE/a-8399

13、77.html 839977Cat. No.: HY-15488A Cat. No.: HY-13954A 438079 (hydrochloride) is a potent, andselective P2X receptor antagonist7with pIC of 6.9.50A 839977 is a P2X7 selective antagonist; itblocks BzATP-evoked calcium influx at recombinanthuman, rat and mouse P2X7 receptors (IC values50are 20 nM, 42 n

14、M and 150 nM respectively) andreduces inflammatory and neuropathic pain inanimal models; the antihyperalgesic effectsPurity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98.74%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK

15、https:/www.MedChemE/A-317491.html A-317491 HYPERLINK https:/www.MedChemE/A-317491.html HYPERLINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html A-317491 HYPERLINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html HYPERLINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html sodium HYPER

16、LINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html HYPERLINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html salt HYPERLINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html HYPERLINK https:/www.MedChemE/A-317491-sodium-salt-hydrate.html hydrateCat. No.: HY-15568 Cat. No.: HY-15568

17、AA-317491 is a potent, selective and non-nucleotideantagonist of P2X and , with3 P2X2/3 receptorsKi hP2X3 rP2X3s of 22, 22, 9, and 92 nM for , ,hP2X2/3 rP2X2/3, and , respectively.A-317491 sodium salt hydrate is a potent,selective and non-nucleotide antagonist of P2X3and P2X receptors, with s of 22,

18、 22, 9,and 92 nM for hP2X3, rP2X3, hP2X2/3, and2/3 KirP2X , respectively.2/3Purity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/a-740003.html A-7

19、40003 HYPERLINK https:/www.MedChemE/a-740003.html HYPERLINK https:/www.MedChemE/A-804598.html A-804598Cat. No.: HY-50697 Cat. No.: HY-100483A-740003 is a potent, selective and competitiveP2X7 receptor antagonist with IC values are 1850and 40 nM for rat and human P2X7 receptors,respectively.A-804598

20、is a CNS penetrant, competitive andselective P2X7 receptor antagonist with IC s of509 nM, 10 nM and 11 nM for mouse, rat and humanP2X7 receptors, respectively.Purity: 98.31%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98.77%Clinical Data: No Development Reporte

21、dSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/AF-353.html AF-353(Ro-4) Cat. No.: HY-14483 HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html Aurintricarboxylic HYPERLINK https:/www.MedChemE/aurintr

22、icarboxylic-acid.html HYPERLINK https:/www.MedChemE/aurintricarboxylic-acid.html acidCat. No.: HY-122575AF-353 (Ro-4) is a potent, selective and orallybioavailable P2X3/P2X2/3 receptor antagonist,with a pIC of 8.0 for both human and rat P2X3,50and with a pIC of 7.3 for human P2X2/3.50Aurintricarboxy

23、lic acid is a nanomolar-potency,allosteric antagonist with selectivity towards-methylene-ATP-sensitive P2X1Rs and P2X3Rs,with IC s of 8.6 nM and 72.9 nM for rP2X1R and50rP2X3R, respectively.Purity: 98.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clin

24、ical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/az10606120-dihydrochloride.html AZ10606120 HYPERLINK https:/www.MedChemE/az10606120-dihydrochloride.html HYPERLINK https:/www.MedChemE/az10606120-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChem

25、E/az10606120-dihydrochloride.html HYPERLINK https:/www.MedChemE/AZD9056-hydrochloride.html AZD9056 HYPERLINK https:/www.MedChemE/AZD9056-hydrochloride.html HYPERLINK https:/www.MedChemE/AZD9056-hydrochloride.html hydrochlorideCat. No.: HY-108669 Cat. No.: HY-19427AAZ10606120 dihydrochloride is a sel

26、ective, highaffinity antagonist for P2X7 receptor (P2X7R)at human and rat with an IC of 10nM.50AZ10606120 dihydrochloride is little or no effectat other P2XR subtypes.AZD9056 hydrochloride is a selective orally activeinhibitor of P2X7 which plays a significant rolein inflammation and pain-causing di

27、seases.Purity: 99.04%Clinical Data:Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98.82%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bay-1797.html BAY-1797 HYPERLINK https:/www.MedChemE/bay-1797.html HYPERLINK https:/www.MedChemE/bullatine-a.ht

28、ml Bullatine HYPERLINK https:/www.MedChemE/bullatine-a.html HYPERLINK https:/www.MedChemE/bullatine-a.html ACat. No.: HY-130605 Cat. No.: HY-N5025BAY-1797 is a potent, orally active, and selectiveP2X4 antagonist, with an IC of 211 nM against50human P2X4. BAY-1797 displays no or very weakactivity on

29、the other P2X ion channels. BAY-1797shows anti-nociceptive and anti-inflammatoryeffects.Bullatine A, a diterpenoid alkaloid of the genusAconitum, possesses anti-rheumatic,anti-inflammatory and anti-nociceptive effects.Purity: 98.66%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg,

30、 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/bx430.html BX430 HYPERLINK https:/www.MedChemE/bx430.html HYPERLINK https:/www.MedChemE/bzatp-tri-triethylammonium.html BzATP HYPERLINK https:/www.MedChemE/bzatp-tri-triethylammonium

31、.html HYPERLINK https:/www.MedChemE/bzatp-tri-triethylammonium.html triethylammonium HYPERLINK https:/www.MedChemE/bzatp-tri-triethylammonium.html HYPERLINK https:/www.MedChemE/bzatp-tri-triethylammonium.html saltCat. No.: HY-110237 Cat. No.: HY-136254BX430 is a potent and selective noncompetitiveal

32、losteric human P2X4 receptor channelsantagonist with an IC of 0.54 M. BX430 has50species specificity. BX430 is used for chronicpain and cardiovascular disease.BzATP triethylammonium salt acts as a P2Xreceptor agonist with pEC s of 8.74, 5.26,507.10, 7.50, 6.19, 6.31, 5.33 for P2X1, P2X2, P2X3,P2X2/3

33、, P2X4 and P2X7, respectively.Purity: 99.87%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 95.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/CE-224535.html CE-224535 HYPERLINK https:/www.MedChemE/CE-224

34、535.html HYPERLINK https:/www.MedChemE/eliapixant.html Eliapixant(PF-04905428) Cat. No.: HY-15487 (BAY 1817080) Cat. No.: HY-109170CE-224535 is a selective P2X receptor7antagonist.Eliapixant (BAY 1817080) is a potent and selectiveantagonist of P2X3 receptor, with an IC of 850nM. Eliapixant can be us

35、ed for the research ofrefractory chronic cough.Purity: 98.88%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.69%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/filapixant.html FilapixantCat. No.: HY-109173 HYPERLINK https:/www

36、.MedChemE/Gefapixant.html Gefapixant(MK-7264; AF-219) Cat. No.: HY-101588Filapixant is a purinoreceptor antagonist extractedfrom patent WO2016091776A1, example 348.Filapixant is the active reference substance ofEliapixant.Gefapixant (MK-7264) is an orally active P2X3receptor (P2X3R) antagonist with

37、IC s of 30 nM50versus recombinant hP2X3 homotrimers and 100-250nM at hP2X2/3 heterotrimeric receptors.Purity: 98.78%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.32%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/ww

38、w.MedChemE/gsk-1482160.html GSK-1482160 HYPERLINK https:/www.MedChemE/gsk-1482160.html HYPERLINK https:/www.MedChemE/GW791343-dihydrochloride.html GW791343 HYPERLINK https:/www.MedChemE/GW791343-dihydrochloride.html HYPERLINK https:/www.MedChemE/GW791343-dihydrochloride.html dihydrochlorideCat. No.:

39、 HY-19888 Cat. No.: HY-15469GSK-1482160 is an orally available negativeallosteric modulator of the P2X7 receptor. P2X7receptors are involved in the production ofpro-inflammatory cytokines, such as Il-1, bycentral and peripheral immune cells.GW791343 dihydrochloride is a P2X7 allostericmodulator; exh

40、ibits species-specific activity andacts as a negative allosteric modulator of humanP2X7 (pIC50 = 6.9 - 7.2).Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.03%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https

41、:/www.MedChemE/GW791343-trihydrochloride.html GW791343 HYPERLINK https:/www.MedChemE/GW791343-trihydrochloride.html HYPERLINK https:/www.MedChemE/GW791343-trihydrochloride.html trihydrochloride HYPERLINK https:/www.MedChemE/GW791343-trihydrochloride.html HYPERLINK https:/www.MedChemE/indophagolin.ht

42、ml IndophagolinCat. No.: HY-15470 Cat. No.: HY-134807GW791343 3Hcl is a P2X7 allosteric modulator;exhibits species-specific activity and acts as anegative allosteric modulator of human P2X7 (pIC50= 6.9 - 7.2).Indophagolin is a potent, indoline-containingautophagy inhibitor (IC =140 nM). Indophagolin

43、50antagonizes the purinergic receptor P2X as well4as P2X and P2X with IC s of 2.71, 2.40 and1 3 503.49 M, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.05%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK ht

44、tps:/www.MedChemE/jnj-42253432.html JNJ-42253432 HYPERLINK https:/www.MedChemE/jnj-42253432.html HYPERLINK https:/www.MedChemE/jnj-47965567.html JNJ-47965567Cat. No.: HY-123481 Cat. No.: HY-101418JNJ-42253432 is a CNS-penetrant, high-affinity andorally active P2X7 antagonist, with pK values ofi9.1 a

45、nd 7.9 for rat and human P2X7 channels,respectively.JNJ-47965567 is a centrally permeable,high-affinity, selective P2X7 antagonist, withpKs of 7.9 and 8.7 for human and rat P2X7,irespectively. JNJ-47965567 can be used to probethe role of central P2X7 in rodent models of CNSpathophysiology.Purity: 98

46、%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/jnj-54166060.html JNJ-54166060 HYPERLINK https:/www.MedChemE/jnj-54166060.html HYPERLINK https:/

47、www.MedChemE/JNJ-54175446.html JNJ-54175446Cat. No.: HY-124300 Cat. No.: HY-117508JNJ-54166060 is a potent and selective P2X7receptor antagonist, with IC s of 4/115/72 nM50for human/rat/mouse P2X7 receptor, respectively.JNJ-54175446 is a potent and selective brainpenetrant P2X7 receptor antagonist,

48、with pIC s50of 8.46 and 8.81 for hP2X7 receptor and rP2X7receptor, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.49%Clinical Data: Phase 2Size: 1 mg, 5 mg, 10 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/jnj-553

49、08942.html JNJ-55308942 HYPERLINK https:/www.MedChemE/jnj-55308942.html HYPERLINK https:/www.MedChemE/KN-62.html KN-62Cat. No.: HY-123857 Cat. No.: HY-13290JNJ-55308942 is a high-affinity, selective,brain-penetrant P2X7 functional antagonist(hP2X7: IC =10 nM, =7.1 nM; rP2X7: =15 nM,50 Ki IC50K=2.9 n

50、M). JNJ-55308942 is orally bioavailable,ibinds to brain P2X7 and blocks IL-1 release fromadult rodent brain.KN-62 is a selective and reversible inhibitor ofcalmodulin-dependent protein kinase II(CaMK-II) with a K of 0.9 M for rat brainiCaMK-II. KN-62 directly binds to the calmodulinbinding site of C

51、aMK-II.Purity: 99.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.45%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Lappaconitine.html Lappaconitine(+)-Lappaconitine) Cat. No.: HY-N0383 HYPERLINK

52、 https:/www.MedChemE/lu-af27139.html Lu HYPERLINK https:/www.MedChemE/lu-af27139.html HYPERLINK https:/www.MedChemE/lu-af27139.html AF27139Cat. No.: HY-132981Lappaconitine, isolated from Aconitum sinomontanumNakai, was characterized as analgesic principle.IC50 value: Target: In vitro: In vivo:Lappac

53、onitine was characterized as analgesicprinciple by our laboratory.Lu AF27139 is a potent, selective, and orallyactive antagonist of P2X7 receptor (IC s of 1250and 2.4 nM for human and rat, Ks of 22, 54, andi13 nM for mouse, human, and rat, respectively). LuAF27139 has rodent-active and CNS-penetrant

54、character.Purity: 98.04%Clinical Data: LaunchedSize: 10 mg, 25 mg, 100 mgPurity: 99.69%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/minodronic-acid.html Minodronic HYPERLINK https:/www.MedChemE/minodronic-acid.html HYPERLINK https:/www.M

55、edChemE/minodronic-acid.html acid(YM-529) Cat. No.: HY-16322 HYPERLINK https:/www.MedChemE/minodronic-acid-d4.html Minodronic HYPERLINK https:/www.MedChemE/minodronic-acid-d4.html HYPERLINK https:/www.MedChemE/minodronic-acid-d4.html acid-d4(YM-529-d4) Cat. No.: HY-16322SMinodronic acid (YM-529) is

56、a third-generationbisphosphonate that directly and indirectlyprevents proliferation, induces apoptosis, andinhibits metastasis of various types of cancercells. Minodronic acid (YM-529) is an antagonistof purinergic P2X2/3 receptors involved in pain.Minodronic acid-d4 is deuterium labeled Minodronica

57、cid. Minodronic acid (YM-529) is athird-generation bisphosphonate that directly andindirectly prevents proliferation, inducesapoptosis, and inhibits metastasis of varioustypes of cancer cells.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical

58、 Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mrs4738.html MRS4738 HYPERLINK https:/www.MedChemE/mrs4738.html HYPERLINK https:/www.MedChemE/nf023-hexasodium.html NF023 HYPERLINK https:/www.MedChemE/nf023-hexasodium.html HYPERLINK https:/www.MedChemE/nf023-hexasodium.ht

59、ml hexasodiumCat. No.: HY-143890 Cat. No.: HY-108676MRS4738 is a potent and high affinity P2Y14Rantagonist. MRS4738 exhibits anti-hyperallodynicand antiasthmatic activity in vivo.NF023 hexasodium is a selective and competitiveP2X receptor1 antagonist, with IC50 values of0.21 M, 28.9 M, 50 M and 100

60、M forhuman P2X , P2X , P2X , and P2X -mediated1 3 2 4responses respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/nf110.html NF110 HYPERLINK https:/www.MedChemE/nf110.html HY