Leukotriene-Receptor-Antagonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html Leukotriene HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html ReceptorLeukotriene Receptor (cys-LTs) are a family of potent bioactive lipids that act through

2、 two structurally divergent G protein-coupledreceptors, termed the CysLT1 and CysLT2 receptors. The cysteinyl leukotrienes LTC4, LTD4, and LTE4 are important mediators ofhuman bronchial asthma. Leukotriene Receptor is a member of the superfamily of G protein-coupled receptors and uses aphosphatidyli

3、nositol-calcium second messenger system. Activation of CysLT1 by LTD4 results in contraction and proliferation ofsmooth muscle, oedema, eosinophil migration and damage to the mucus layer in the lung. Leukotriene receptor antagonists, calledLTRAs for short, are a class of oral medication that is non-

4、steroidal. They may also be referred to as anti-inflammatorybronchoconstriction preventors. LTRAs work by blocking a chemical reaction that can lead to inflammation in the airways.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html Leukotriene HYPERLINK https:/www.MedChemE

5、/Targets/Leukotriene Receptor.html HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Leukotriene Re

6、ceptor.html HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html Agonists HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Leukotriene Receptor.html HYPERLINK https:/www.

7、MedChemE/Targets/Leukotriene Receptor.html Antagonists HYPERLINK https:/www.MedChemE/hami-3379.html (Rac)-HAMI HYPERLINK https:/www.MedChemE/hami-3379.html HYPERLINK https:/www.MedChemE/hami-3379.html 3379Cat. No.: HY-112248 HYPERLINK https:/www.MedChemE/s-verapamil-d7-hydrochloride.html (S)-Verapam

8、il HYPERLINK https:/www.MedChemE/s-verapamil-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/s-verapamil-d7-hydrochloride.html D7 HYPERLINK https:/www.MedChemE/s-verapamil-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/s-verapamil-d7-hydrochloride.html hydrochloride(S)-(-)-Verapamil D7 hydr

9、ochloride) Cat. No.: HY-135336AS(Rac)-HAMI 3379 is the racemate of HAMI 3379. HAMI3379 is a potent and selective Cysteinylleukotriene (CysLT ) receptor antagonist.2(S)-Verapamil D7 hydrochloride (S)-(-)-VerapamilD7 hydrochloride) is a deuterium labeled(S)-Verapamil hydrochloride. (S)-Verapamilhydroc

10、hloride (S(-)-Verapamil hydrochloride)inhibits leukotriene C4 (LTC4) and calceintransport by MRP1.Purity: 95.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/s-verapamil-hydrochloride.html (S)-Ve

11、rapamil HYPERLINK https:/www.MedChemE/s-verapamil-hydrochloride.html HYPERLINK https:/www.MedChemE/s-verapamil-hydrochloride.html hydrochloride(S)-(-)-Verapamil hydrochloride) Cat. No.: HY-135336A HYPERLINK https:/www.MedChemE/s-s-verapamil-d6-hydrochloride.html (S)-Verapamil-d6 HYPERLINK https:/www

12、.MedChemE/s-s-verapamil-d6-hydrochloride.html HYPERLINK https:/www.MedChemE/s-s-verapamil-d6-hydrochloride.html hydrochloride(S)-(-)-Verapamil-d6 hydrochloride) Cat. No.: HY-135336AS1(S)-Verapamil hydrochloride (S(-)-Verapamilhydrochloride) inhibits leukotriene C4 (LTC4) andcalcein transport by MRP1

13、. (S)-Verapamilhydrochloride leads to the death of potentiallyresistant tumor cells.(S)-Verapamil-d6 (S)-(-)-Verapamil-d6)hydrochloride is the deuterium labeled(S)-Verapamil hydrochloride. (S)-Verapamilhydrochloride (S(-)-Verapamil hydrochloride)inhibits leukotriene C4 (LTC4) and calceintransport by

14、 MRP1.Purity: 99.39%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/11-keto-beta-boswellic-acid.html 11-Keto-beta-boswellic HYPERLINK https:/www.MedChemE/11-keto-beta-boswellic-acid.ht

15、ml HYPERLINK https:/www.MedChemE/11-keto-beta-boswellic-acid.html acid(11-Keto-boswellic acid) Cat. No.: HY-N2056 HYPERLINK https:/www.MedChemE/12s-hht.html 12S-HHT(12(S)-HHTrE) Cat. No.: HY-11333011-Keto-beta-boswellic acid (11-Keto-boswellicacid) is a pentacyclic triterpenic acid of theoleogum res

16、in from the bark of the Boswelliaserrate tree, popularly known as IndianFrankincense.12S-HHT (12(S)-HHTrE) is an enzymatic product ofprostaglandin H (PGH ) derived from2 2cyclooxygenase (COX)-mediated arachidonic acidmetabolism. 12S-HHT is an endogenous ligand forBLT2 that fully activates BLT2 in vi

17、vo.Purity: 99.96%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/5-o-demethylnobiletin.html 5-O-Demethylnobiletin HYPERLINK https:/www.MedChemE/5-o-demethylnobiletin.html HYPERLINK https:/www.Med

18、ChemE/ablukast.html Ablukast(5-Demethylnobiletin) Cat. No.: HY-N1942 (Ro 23-3544) Cat. No.: HY-1189585-O-Demethylnobiletin (5-Demethylnobiletin), apolymethoxyflavone isolated from Sideritistragoriganum, is a direct inhibition of 5-LOX(IC =0.1 M), without affecting the expression of50COX-2.Ablukast (

19、Ro 23-3544) is a specific and activeleukotriene receptor antagonist. Ablukasteffectively reduces LTC4- and antigen-inducedbronchoconstriction. Ablukast is LTD4 receptorantagonist.Purity: 99.93%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 99.36%Clinical Data: No Development R

20、eportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Amelubant.html Amelubant HYPERLINK https:/www.MedChemE/Amelubant.html HYPERLINK https:/www.MedChemE/AS-35.html AS-35(BIIL 284) Cat. No.: HY-19304Cat. No.: HY-101946Amelubant (BIIL 284) is a potent, oral and longacting

21、 LTB receptor antagonist, negligibly4binds to LTB4 receptor, with Kis of 221 nM and230 nM in vital cells and membranes. Amelubant(BIIL 284) is a prodrug of active metabolites BIIL260 and BIIL 315. Anti-inflammatory activity.AS-35 is an orally effective, potent and selectiveantagonist of leukotrienes

22、, antagonizes LTC4-, LTD4and LTE4-induced contractions of the ileum withIC values of 8 nM, 4 nM and 3 nM, respectively,50and has antiallergic activities.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-68

23、98 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/bay-u-9773.html BAY-u HYPERLINK https:/www.MedChemE/bay-u-9773.html HYPERLINK https:/www.MedChemE/bay-u-9773.html 9773 HYPERLINK https:/www.MedChemE/bay-u-9773.html HYPERLINK https:/www.MedChemE/biil-260-hydrochloride.html BIIL-

24、260 HYPERLINK https:/www.MedChemE/biil-260-hydrochloride.html HYPERLINK https:/www.MedChemE/biil-260-hydrochloride.html hydrochlorideCat. No.: HY-107609 Cat. No.: HY-114641ABAY-u 9773 is a non-selective antagonist of theCysLT receptors (cysteinyl leukotrienesreceptors) with about the same IC for Cys

25、LT and150CysLT2. BAY-u9773 is used for the inhibition ofLT responses.BIIL-260 hydrochloride is a potent and long-actingorally active leukotriene B(4) receptor LTB4antagonist, with anti-inflammatory activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.0%Clinical Data:

26、No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg HYPERLINK https:/www.MedChemE/U66858.html Bunaprolast(U66858) Cat. No.: HY-U00170 HYPERLINK https:/www.MedChemE/cay10583.html CAY10583Cat. No.: HY-122124Bunaprolast (U66858) is a potent inhibitor ofLTB production in human whole blood.4Bunaprolast (

27、U66858) also exhibits significantinhibition of lipoxygenase and TXB release.2CAY10583 is a potent and selective fullLeukotriene B4 receptor type 2 (BLT2) agonist.CAY10583 directly promotes keratinocyte migrationin vitro and accelerates wound closure in vivo.CAY10583 is a promising pharmaceutical age

28、nt fordiabetic wounds.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/1H-Indole-2-carboxamide,_5-methoxy-3-_1-methylethoxy_-1-phenyl-N-2H-tetrazol-5-yl-.html CI-949Cat. No.: HY-U00364 HYP

29、ERLINK https:/www.MedChemE/CP-105696.html CP-105696(Pfizer 105696) Cat. No.: HY-19193CI-949 is an allergic mediator release inhibitor,which inhibits histamine, leukotriene C /D4 4(LTC4/LTD4), and thromboxane B2 (TXB2)release with IC s of 11.4 M, 0.5 M and 0.1 M,50respectively.CP-105696 is a potent a

30、nd selective LeukotrieneB4 Receptor antagonist, with an IC50 of 8.42 nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/cp-96021-hydrochloride.html CP-96021 HYPERLINK https:/www.MedChemE/cp-

31、96021-hydrochloride.html HYPERLINK https:/www.MedChemE/cp-96021-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/cp-96021-hydrochloride.html HYPERLINK https:/www.MedChemE/CP-96486.html CP-96486Cat. No.: HY-101731 Cat. No.: HY-100316CP-96021 hydrochloride is a balanced, combined,potent

32、and orally active leukotriene D4(LTD4)/platelet activating factor (PAF) receptorantagonist with K values of 34 nM and 37 nM,irespectively.CP-96486 is a potent and orally active leukotrieneD4 (LTD4)/platelet activating factor (PAF)receptor antagonist with Ks of 20 and 24 nM,irespectively.Purity: 98%C

33、linical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/darbufelone.html Darbufelone HYPERLINK https:/www.MedChemE/darbufelone.html HYPERLINK https:/www.MedChemE/Darbufelone_(mesylate).html Darbufelone HYPER

34、LINK https:/www.MedChemE/Darbufelone_(mesylate).html HYPERLINK https:/www.MedChemE/Darbufelone_(mesylate).html mesylate(CI-1004) Cat. No.: HY-101438 (CI-1004 mesylate) Cat. No.: HY-101438ADarbufelone is a dual inhibitor of cellularPGF and production. Darbufelone2 LTB4potently inhibits PGHS-2 (IC = 0

35、.19 M) but is50much less potent with PGHS-1 (IC =20 M).50Darbufelone mesylate (CI-1004 mesylate) is a dualinhibitor of cellular PGF2 and LTB4production. Darbufelone potently inhibits PGHS-2(IC = 0.19 M) but is much less potent with50PGHS-1 (IC = 20 M).50Purity: 98.0%Clinical Data: No Development Rep

36、ortedSize: 1 mgPurity: 98.45%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/DW-1350.html DW-1350Cat. No.: HY-100173 HYPERLINK https:/www.MedChemE/etalocib.html Etalocib(LY293111; VML 295) Cat. No.: HY-13628DW-1350 is a LTB re

37、ceptor antagonist.4Etalocib (LY293111), an orally active leukotrieneB receptor antagonist, inhibits the binding of43HLTB , with a of 25 nM. Etalocib4 Ki(LY293111) prevents LTB -induced calcium4mobilization with an lC of 20 nM. Etalocib50(LY293111) induces apoptosis.Purity: 98%Clinical Data: No Devel

38、opment ReportedSize: 1 mg, 5 mgPurity: 98.27%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GSK2190915.html Fiboflapon(GSK2190915; AM-803) Cat. No.: HY-15874 HYPERLINK https:/www.MedChemE/GSK2190915-sodium-salt.html Fiboflapon HYPERLINK ht

39、tps:/www.MedChemE/GSK2190915-sodium-salt.html HYPERLINK https:/www.MedChemE/GSK2190915-sodium-salt.html sodium(GSK2190915 sodium salt; AM-803 sodium) Cat. No.: HY-15874AFiboflapon (GSK2190915; AM-803) is a potent andorally bioavailable 5-lipoxygenase-activatingprotein (FLAP) inhibitor with a potency

40、 of 2.9 nMin FLAP binding, an IC of 76 nM for inhibition50of LTB4 in human blood.Fiboflapon sodium (GSK2190915; AM-803) is a potentand orally bioavailable 5-lipoxygenase-activatingprotein (FLAP) inhibitor with a potency of 2.9 nMin FLAP binding, an IC of 76 nM for inhibition50of LTB4 in human blood.

41、Purity: 98.54%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.91%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Gemilukast.html Gemilukast(ONO-6950) Cat. No.: HY-16780 HYPERLINK https:/www.MedChemE/gpbar1-in-3.html GPBAR1-IN-3Cat. No.: H

42、Y-145234Gemilukast is an orally active and potent dualcysteinyl leukotriene 1 and 2 receptors (CysLT1and CysLT2) IC50santagonist, with of 1.7, 25 nMfor human CysLT and CysLT , respectively.1 2GPBAR1-IN-3 (Compound 14) is a selective GPBAR1agonist (EC =0.17 M) and a CysLT R50 1antagonist.Purity: 99.5

43、8%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hami-3379-1.html HAMI HYPERLINK https:/www.MedChemE/hami-3379-1.html HYPERLINK https:/www.MedChemE/hami-3379-1.html 3379

44、 HYPERLINK https:/www.MedChemE/hami-3379-1.html HYPERLINK https:/www.MedChemE/KP496.html KP496Cat. No.: HY-112248A Cat. No.: HY-U00253HAMI 3379 is a potent and selective CysLT2receptor antagonist. HAMI 3379 has a protectiveeffect on acute and subacute ischemic braininjury, and attenuates microglia-r

45、elatedinflammation.KP496 is a selective, dual antagonist forLeukotriene D4 receptor and Thromboxane A2receptor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.81%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/5,12-DiHETE.html Leukotriene HY

46、PERLINK https:/www.MedChemE/5,12-DiHETE.html HYPERLINK https:/www.MedChemE/5,12-DiHETE.html B4 HYPERLINK https:/www.MedChemE/5,12-DiHETE.html HYPERLINK https:/www.MedChemE/leukotriene-b4-d4.html Leukotriene HYPERLINK https:/www.MedChemE/leukotriene-b4-d4.html HYPERLINK https:/www.MedChemE/leukotrien

47、e-b4-d4.html B4-d4(LTB4; 5(S),12(R)-DiHETE) Cat. No.: HY-107608 (LTB4-d4; 5(S),12(R)-DiHETE-d4) Cat. No.: HY-107608SLeukotriene B4 (LTB4) is known as one of the mostpotent chemoattractants and activators ofleukocytes and is involved in inflammatorydiseases. Leukotriene B4 is also an alkylchain-based

48、 PROTAC linker that can be used in thesynthesis of PROTACs.Leukotriene B4-d4 (LTB4-d4) is the deuteriumlabeled Leukotriene B4. Leukotriene B4 (LTB4) isknown as one of the most potent chemoattractantsand activators of leukocytes and is involved ininflammatory diseases.Purity: 98.0%Clinical Data: Phas

49、e 2Size: 25 g (297.2 M * 250 L in Ethanol)Purity: 98%Clinical Data: No Development ReportedSize: 25 g4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/leukotriene-f4.html Leukotriene HYPERLINK https:/www.MedChemE/leukotriene-f4.html HYPERLINK https:/www.MedChem

50、E/leukotriene-f4.html F4 HYPERLINK https:/www.MedChemE/leukotriene-f4.html HYPERLINK https:/www.MedChemE/LM-1484.html LM-1484Cat. No.: HY-130440 Cat. No.: HY-101686Leukotriene F4 (LTF4), is a lipid that belongs tothe Cysteinyl Leukotriene (CysTL) family.Leukotriene F4 induces bronchoconstriction wit

51、h anED of 16 g/kg. The precursor of LTF4 is50Leukotriene E4 (LTE4), which isformed from theaction of a glutamyl transferase.LM-1484 is an antagonist of CysLT1 receptor anddisplays a higher affinity for 3H-LTC4 sites.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical

52、 Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Cycloheptaneacetamide,_N-_methylsulfonyl_-_alpha_-4-_2-quinolinylmethoxy_phenyl-.html LTB4-IN-1 HYPERLINK https:/www.MedChemE/Cycloheptaneacetamide,_N-_methylsulfonyl_-_alpha_-4-_2-quinolinylmethoxy_phenyl-.html HYPERLINK h

53、ttps:/www.MedChemE/1H-Indole-5-carboxamide,_3-2-methoxy-4-_2-methylphenyl_sulfonylaminocarbonylphenylmethyl-1-methyl-N-_4,4,4-trifluoro-2-methylbutyl_-.html LTD4 HYPERLINK https:/www.MedChemE/1H-Indole-5-carboxamide,_3-2-methoxy-4-_2-methylphenyl_sulfonylaminocarbonylphenylmethyl-1-methyl-N-_4,4,4-t

54、rifluoro-2-methylbutyl_-.html HYPERLINK https:/www.MedChemE/1H-Indole-5-carboxamide,_3-2-methoxy-4-_2-methylphenyl_sulfonylaminocarbonylphenylmethyl-1-methyl-N-_4,4,4-trifluoro-2-methylbutyl_-.html antagonist HYPERLINK https:/www.MedChemE/1H-Indole-5-carboxamide,_3-2-methoxy-4-_2-methylphenyl_sulfon

55、ylaminocarbonylphenylmethyl-1-methyl-N-_4,4,4-trifluoro-2-methylbutyl_-.html HYPERLINK https:/www.MedChemE/1H-Indole-5-carboxamide,_3-2-methoxy-4-_2-methylphenyl_sulfonylaminocarbonylphenylmethyl-1-methyl-N-_4,4,4-trifluoro-2-methylbutyl_-.html 1Cat. No.: HY-U00299 Cat. No.: HY-U00359LTB4-IN-1 (Comp

56、ound 6) is a leukotriene synthesis(LTB4) inhibitor with an IC of 70 nM.50LTD antagonist 1 is a potent, orally active4antagonist of leukotriene D4 (LTD4) with a Kiof 0.57 nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

57、 mg HYPERLINK https:/www.MedChemE/LY210073.html LY210073Cat. No.: HY-U00263 HYPERLINK https:/www.MedChemE/LY223982.html LY223982(CGS23131; SKF107324) Cat. No.: HY-112737LY210073 is a Leukotriene B4 (LTB4) receptorantagonist with an IC of 6.2 nM.50LY223982 is a potent and specific inhibitor ofleukotr

58、iene B4 receptor, with an IC of 13.2 nM50against 3HLTB4 binding to LTB4 receptor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 100.0%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/ly255283.html LY255283 HYPERLINK https:/www.MedChemE/ly255283

59、.html HYPERLINK https:/www.MedChemE/masilukast.html MasilukastCat. No.: HY-15744(ZD-3523) Cat. No.: HY-105221LY255283 is a LTB receptor (BLT2) antagonist,4with an IC of 100 nM for 3HLTB binding to50 4guinea pig lung membranes.Masilukast is an orally administered cysteinylleukotriene D (LTD ) recepto

60、r antagonist with4 4potential to treat asthma.Purity: 98.73%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/MK-571-sodium-salt.html MK-571 HYPERLINK https:/www.Med