Protease-Activated-Receptor-PAR-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Protease-Activated HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Receptor HYPERLINK https:/www.MedChemE/Targets/Pr

2、otease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html (PAR)Thrombin receptorsProtease activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) that are irreversibly activated byproteolytic cleavage of the N terminus, w

3、hich unmasks a tethered peptide ligand that binds and activates the transmembranereceptor domain, eliciting a cellular cascade in response to inflammatory signals and other stimuli. There are four members of thePAR family: PAR1, PAR2, PAR3 and PAR4. PARs have important functions in the vasculature,

4、inflammation, and cancer and areimportant drug targets.PARs are expressed on nearly all cell types in the blood vessel wall (ECs, fibroblasts, myocytes) and blood (platelets, neutrophils,macrophages, leukemic white cells) with exception of red blood cells. Thrombin-activated PAR-1, PAR-3, and PAR-4

5、are alsoexpressed in epithelium, neurons, astrocytes, and immune cells. PAR-2, which is activated by trypsin-like serine proteases, is foundin human vascular, intestinal, neuronal, and airway cells. Its expression increases in injured tissues or after stimulation byinflammatory mediators.www.MedChem

6、E 1 HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Protease-Activated HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Receptor HYPERLINK https:/www.MedChemE/Targets

7、/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html (PAR) HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Inhibitors, HYPERLINK h

8、ttps:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Agonists HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR)

9、.html & HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html HYPERLINK https:/www.MedChemE/Targets/Protease-Activated Receptor (PAR).html Antagonists HYPERLINK https:/www.MedChemE/2-furoyl-ligrlo-amide.html 2-Furoyl-LIGRLO-amide HYPERLINK https:/www.MedChemE/2-furoyl-ligrlo-a

10、mide.html HYPERLINK https:/www.MedChemE/2-furoyl-ligrlo-amide-tfa.html 2-Furoyl-LIGRLO-amide HYPERLINK https:/www.MedChemE/2-furoyl-ligrlo-amide-tfa.html HYPERLINK https:/www.MedChemE/2-furoyl-ligrlo-amide-tfa.html TFACat. No.: HY-P1314 Cat. No.: HY-P1314A2-Furoyl-LIGRLO-amide is a potent and select

11、iveproteinase-activated receptor 2 (PAR2) agonistwith a pD value of 7.0.22-Furoyl-LIGRLO-amide TFA is a potent andselective proteinase-activated receptor 2 (PAR2)agonist with a pD value of 7.0.2Purity: 99.87%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No De

12、velopment ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/ac-264613.html AC-264613 HYPERLINK https:/www.MedChemE/ac-264613.html HYPERLINK https:/www.MedChemE/AC-55541.html AC-55541Cat. No.: HY-14351 Cat. No.: HY-14350AC-264613 is a potent and selectiveprotease-activated receptor (PAR-2

13、) agonist witha pEC of 7.5.50AC-55541 is a highly selective protease-activatedreceptor 2 (PAR2) agonist (pEC =6.7), displays50no activity at other PAR subtypes or at over 30other receptors involved in nociception andinflammation.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity

14、: 99.19%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/atopaxar.html Atopaxar(E5555; ER-172594-00) Cat. No.: HY-18200 HYPERLINK https:/www.MedChemE/atopaxar-hydrobromide.html Atopaxar HYPERLINK https:/www.MedChemE/atopaxar-hydrobromide.html H

15、YPERLINK https:/www.MedChemE/atopaxar-hydrobromide.html hydrobromide(E5555 hydrobromide; ER 172594-06) Cat. No.: HY-18200BAtopaxar (E5555) is a potent, orally active,selective and reversible thrombin receptorprotease-activated receptor-1 (PAR-1) antagonist.Atopaxar, an antiplatelet agent, interferes

16、 withplatelet signaling. Atopaxar can be used for theresearch of atherothrombotic disease.Atopaxar (E5555) hydrobromide is a potent, orallyactive, selective and reversible thrombin receptorprotease-activated receptor-1 (PAR-1) antagonist.Atopaxar hydrobromide, an antiplatelet agent,interferes with p

17、latelet signaling.Purity: 98.05%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZ3451.html AZ3451 HYPERLINK https:/www.MedChemE/AZ3451.html HYPERLINK https:/www.MedChemE/BMS-986120.html BMS-

18、986120Cat. No.: HY-112558 Cat. No.: HY-19837AZ3451 is a potent protease-activated receptor-2(PAR2) antagonist with IC of 23 nM.50BMS-986120 is a first-in-class oral and reversibleprotease-activated receptor 4 (PAR4) antagonist,with IC s of 9.5 nM and 2.1 nM in human and50monkey blood, respectively.

19、BMS-986120 has potentand selective antiplatelet effects.Purity: 99.60%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: Phase 1Size: 5 mg HYPERLINK https:/www.MedChemE/cbk289001.html CBK289001 HYPERLINK https:/www.MedChemE/cbk289001.

20、html HYPERLINK https:/www.MedChemE/enmd-1068-hydrochloride.html ENMD-1068 HYPERLINK https:/www.MedChemE/enmd-1068-hydrochloride.html HYPERLINK https:/www.MedChemE/enmd-1068-hydrochloride.html hydrochlorideCat. No.: HY-124663 Cat. No.: HY-124748ACBK289001 is a tartrate-resistant acid phosphatase(TRAP

21、/ACP5) inhibitor. CBK289001 inhibits TRAP5bMV, TRAP 5bOX and TRAP 5aOX with IC s50of 125 M, 4.21 M and 14.2 M, respectively.ENMD-1068 hydrochloride is a selectiveprotease-activated receptor 2 (PAR2) antagonistwith antiangiogenic and anti-inflammatoryactivities.Purity: 98%Clinical Data: No Developmen

22、t ReportedSize: 1 mg, 5 mgPurity: 98.18%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/fr-171113.html FR-171113 HYPERLINK https:/www.MedChemE/fr-171113.html HYPERLINK https:/www

23、.MedChemE/fsllry-nh2.html FSLLRY-NH2Cat. No.: HY-108555 Cat. No.: HY-P1260FR171113 is a specific and non-peptide thrombinreceptor antagonist. FR171113 exhibits theantithrombotic effects of a PAR1 antagonist.FR171113 inhibits thrombin-induced plateletaggregation with an IC of 0.29 M.50FSLLRY-NH2 is a

24、 protease-activated receptor 2(PAR2) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fsllry-nh2-tfa.html FSLLRY-NH2 HYPERLINK https:/www.MedChemE/fsllry-nh2-tfa.html HYPERLINK h

25、ttps:/www.MedChemE/fsllry-nh2-tfa.html TFA HYPERLINK https:/www.MedChemE/fsllry-nh2-tfa.html HYPERLINK https:/www.MedChemE/gb-110.html GB-110Cat. No.: HY-P1260A Cat. No.: HY-120528FSLLRY-NH2 TFA is a protease-activated receptor 2(PAR2) inhibitor.GB-110 is a potent, orally active, and nonpeptidicprot

26、ease activated receptor 2 (PAR2) agonist.GB-110 selectively induces PAR2-mediatedintracellular Ca2+ release in HT29 cells with anEC of 0.28 M.50Purity: 98.20%Clinical Data: No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChem

27、E/gb-110-hydrochloride.html GB-110 HYPERLINK https:/www.MedChemE/gb-110-hydrochloride.html HYPERLINK https:/www.MedChemE/gb-110-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/gb-110-hydrochloride.html HYPERLINK https:/www.MedChemE/gb-88.html GB-88Cat. No.: HY-120528A Cat. No.: HY-120

28、261GB-110 hydrochloride is a potent, orally active,and nonpeptidic protease activated receptor 2(PAR2) agonist. GB-110 hydrochloride selectivelyinduces PAR2-mediated intracellular Ca2+ releasein HT29 cells with an EC of 0.28 M.50GB-88 is an oral, selective non-peptide antagonistof PAR2, inhibits PAR

29、2 activated Ca2+ releasewith an IC of 2 M.50Purity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/i-191.html I-191 HY

30、PERLINK https:/www.MedChemE/i-191.html HYPERLINK https:/www.MedChemE/ml354.html ML354Cat. No.: HY-117793(VU0099704) Cat. No.: HY-19973I-191 is a potent, selective protease-activatedreceptor 2 (PAR2) antagonist.ML354 is a selective PAR4 antagonist with an IC50of 140 nM.Purity: 99.38%Clinical Data: No

31、 Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html PAR HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html 4 HYPERLINK

32、 https:/www.MedChemE/par-4-1-6-tfa.html HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html (1-6) HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html (TFA) HYPERLINK https:/www.MedChemE/par-4-1-6-tfa.html HYPERLINK https:/www.MedChemE/par-2-in-1.html PAR-2-

33、IN-1(GYPGQV TFA) Cat. No.: HY-P1313ACat. No.: HY-138558PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is afragment of protease-activated receptor 4 (PAR ).4PAR 4 (1-6) TFA acts as a PAR -specific agonist.4PAR-2-IN-1 is a protease-activated receptor-2(PAR2) signaling pathway inhibitor withanti-inflamma

34、tory and anticancer effects.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.16%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide.html PAR-4 HYPERLINK https:/www.MedChemE/P

35、AR-4_Agonist_Peptide,_amide.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide.html Agonist HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide.html Peptide, HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide

36、.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide.html amide(PAR-4-AP; AY-NH2) Cat. No.: HY-P1309 HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html PAR-4 HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_P

37、eptide,_amide_TFA.html Agonist HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html Peptide, HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_ami

38、de_TFA.html amide HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html HYPERLINK https:/www.MedChemE/PAR-4_Agonist_Peptide,_amide_TFA.html TFA(PAR-4-AP TFA; AY-NH2 TFA) Cat. No.: HY-P1309APAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) isa proteinase-activated receptor-4 (PAR-4)agonis

39、t, which has no effect on either PAR-1 orPAR-2 and whose effects are blocked by a PAR-4antagonist.PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA;AY-NH2 TFA) is a proteinase-activated receptor-4(PAR-4) agonist, which has no effect on eitherPAR-1 or PAR-2 and whose effects are blocked by aPAR-4 antago

40、nist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 99.93%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/parmodulin-2.html Parmodulin HYPERLINK https:/www.MedChemE/parmodulin-2.html HYPERLINK https:/www.MedChemE/parmodulin

41、-2.html 2(ML161) Cat. No.: HY-13965 HYPERLINK https:/www.MedChemE/parstatin-human.html Parstatin(human)Cat. No.: HY-P1262Parmodulin 2 (ML161) is an allosteric inhibitor ofprotease-activated receptor 1 (PAR1) with an ICof 0.26 M.50Parstatin(human), a cell-penetrating PAR-1thrombin receptor agonist pe

42、ptide, is a potentinhibitor of angiogenesis.Purity: 98.03%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/parstatin-human-tfa.html Parstatin(human) HYPERLINK https

43、:/www.MedChemE/parstatin-human-tfa.html HYPERLINK https:/www.MedChemE/parstatin-human-tfa.html TFA HYPERLINK https:/www.MedChemE/parstatin-human-tfa.html HYPERLINK https:/www.MedChemE/parstatin-mouse.html Parstatin(mouse)Cat. No.: HY-P1262A Cat. No.: HY-P1261Parstatin(human) TFA, a cell-penetrating

44、PAR-1thrombin receptor agonist peptide, is a potentinhibitor of angiogenesis.Parstatin(mouse), a cell-penetrating PAR-1thrombin receptor agonist peptide, is a potentinhibitor of angiogenesis.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Rep

45、ortedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/parstatin-mouse-tfa.html Parstatin(mouse) HYPERLINK https:/www.MedChemE/parstatin-mouse-tfa.html HYPERLINK https:/www.MedChemE/parstatin-mouse-tfa.html TFA HYPERLINK https:/www.MedChemE/parstatin-mouse-tfa.html HYPERLINK https:/www.MedChemE/proteas

46、e-activated-receptor-1-par-1-agonist.html Protease-Activated HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist.html Receptor-1, HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-ago

47、nist.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist.html PAR-1 HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist.html AgonistCat. No.: HY-P1261A Cat. No.: HY-P2518Pa

48、rstatin(mouse) TFA, a cell-penetrating PAR-1thrombin receptor agonist peptide, is a potentinhibitor of angiogenesis.Protease-Activated Receptor-1, PAR-1 Agonist is aselective proteinase-activated receptor1 (PAR-1)agonist peptide. Protease-Activated Receptor-1,PAR-1 Agonist corresponds to PAR1 tether

49、ed ligandand which can selectively mimic theactions ofthrombin via this receptor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html Prote

50、ase-Activated HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html Receptor-1, HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html HYPERLINK https:/www.MedC

51、hemE/protease-activated-receptor-1-par-1-agonist-tfa.html PAR-1 HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html Agonist HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-pa

52、r-1-agonist-tfa.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html TFA HYPERLINK https:/www.MedChemE/protease-activated-receptor-1-par-1-agonist-tfa.html HYPERLINK https:/www.MedChemE/Protease-Activated_Receptor-2,_amide.html Protease-Activated HYPERLINK https:/w

53、ww.MedChemE/Protease-Activated_Receptor-2,_amide.html HYPERLINK https:/www.MedChemE/Protease-Activated_Receptor-2,_amide.html Receptor-2, HYPERLINK https:/www.MedChemE/Protease-Activated_Receptor-2,_amide.html HYPERLINK https:/www.MedChemE/Protease-Activated_Receptor-2,_amide.html amideCat. No.: HY-

54、P2518A Cat. No.: HY-P0283Protease-Activated Receptor-1, PAR-1 Agonist TFAis a selective proteinase-activated receptor1(PAR-1) agonist peptide. Protease-ActivatedReceptor-1, PAR-1 Agonist TFA corresponds to PAR1tethered ligand and which can selectively mimictheactions of thrombin via this receptor.Pr

55、otease-Activated Receptor-2, amide (SLIGKV-NH )2is a highly potent protease-activated receptor-2(PAR2) activating peptide.Purity: 99.08%Clinical Data: No Development ReportedSize: 10 mgPurity: 98.48%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg4 Tel: 609-228-6898 Fax: 60

56、9-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html Protease-Activated HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html Recept

57、or-3 HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html (PAR-3) HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html HYPERLINK https:/www.MedChemE/protease-activ

58、ated-receptor-3-par-3-1-6-human.html (1-6), HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html human HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human.html HYPERLI

59、NK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human-tfa.html Protease-Activated HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human-tfa.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human-tfa.html Receptor-3 HYPERLINK https:/www.M

60、edChemE/protease-activated-receptor-3-par-3-1-6-human-tfa.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human-tfa.html (PAR-3) HYPERLINK https:/www.MedChemE/protease-activated-receptor-3-par-3-1-6-human-tfa.html HYPERLINK https:/www.MedChemE/protease-activated-receptor-3