LPL-Receptor-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html LPL HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html ReceptorLysophospholipid ReceptorLPL Receptor (Lysophospholipid Receptor) group are members of the G protein-coupled receptor f

2、amily of integral membraneproteins that are important for lipid signaling. In humans, there are eight LPL receptors, each encoded by a separate gene. TheseLPL receptor genes are also sometimes referred to as Edg. LPL receptor ligands bind to and activate their cognate receptorslocated in the cell me

3、mbrane. Depending on which ligand, receptor, and cell type is involved, the activated receptor can have arange of effects on the cell. These include primary effects of inhibition of adenylyl cyclase and release of calcium from theendoplasmic reticulum, as well as secondary effects of preventingapopt

4、osis and increasing cell proliferation. Type: LPAR1, LPAR2,LPAR3, LPAR4, LPAR5, LPAR6, S1PR1, S1PR2, S1PR3, S1PR4, S1PR5.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html LPL HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Recept

5、or.html Receptor HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets

6、/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html Activators HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Tar

7、gets/LPL Receptor.html & HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html HYPERLINK https:/www.MedChemE/Targets/LPL Receptor.html Modulators HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid.html 1-Oleoyl HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid.html HYPERLINK h

8、ttps:/www.MedChemE/1-oleoyl-lysophosphatidic-acid.html lysophosphatidic HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid.html HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid.html acid(1-Oleoyl-sn-glycero-3-phosphate; 1-Oleoyl-LPA) Cat. No.: HY-137862 HYPERLINK https:/www.Med

9、ChemE/1-oleoyl-lysophosphatidic-acid-sodium.html 1-Oleoyl HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid-sodium.html HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid-sodium.html lysophosphatidic HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid-sodium.html HYPERL

10、INK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid-sodium.html acid HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid-sodium.html HYPERLINK https:/www.MedChemE/1-oleoyl-lysophosphatidic-acid-sodium.html sodium(1-Oleoyl-sn-glycero-3-phosphate sodium; ) Cat. No.: HY-1076141-Oleoyl lysop

11、hosphatidic acid(1-Oleoyl-sn-glycero-3-phosphate) is an abundantlysophosphatidic acid (LPA) species with highbiological activity due to its strong affinity forthe LPA receptors.1-Oleoyl lysophosphatidic acid(1-Oleoyl-sn-glycero-3-phosphate) sodium, a potentbioactive phospholipid, is a LPA receptorac

12、tivator. 1-Oleoyl lysophosphatidic acid sodiumcan promote mitosis by inducing DNA synthesis.Purity: 95.0%Clinical Data: No Development ReportedSize: 10 mg (22.91 mM * 1 mL in Ethanol)Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/4-deoxypyr

13、idoxine-5-phosphate.html 4-Deoxypyridoxine HYPERLINK https:/www.MedChemE/4-deoxypyridoxine-5-phosphate.html HYPERLINK https:/www.MedChemE/4-deoxypyridoxine-5-phosphate.html 5-phosphate HYPERLINK https:/www.MedChemE/4-deoxypyridoxine-5-phosphate.html HYPERLINK https:/www.MedChemE/a6770.html A6770Cat.

14、 No.: HY-N2553 Cat. No.: HY-1390944-Deoxypyridoxine 5-phosphate is a Pyridoxal5-phosphate analogue and a sphingosine 1-phosphate(S1P) inhibitor. 4-Deoxypyridoxine 5-phosphateinhibits ornithine decarboxylase activity with a Kiof 60 M.A6770 is an orally active, potent sphingosine1-phosphate (S1P) lyas

15、e (S1PL) inhibitor. A6770is phosphorylated and the phosphorylated formdirectly inhibits S1P lyased.A6770, a potentialkey metabolite of THI, induces a 3HdhS1Pincrease.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Developmen

16、t ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AM095.html AM095 HYPERLINK https:/www.MedChemE/AM095.html HYPERLINK https:/www.MedChemE/AM095-free-acid.html AM095 HYPERLINK https:/www.MedChemE/AM095-free-acid.html HYPERLINK https:/www.MedChemE/AM095-free-acid.html free HYPERLINK https:/www.

17、MedChemE/AM095-free-acid.html HYPERLINK https:/www.MedChemE/AM095-free-acid.html acidCat. No.: HY-16039 Cat. No.: HY-16040AM095 is a selective LPA receptor antagonist.1The IC for AM095 antagonism of LPA-induced50calcium flux of human or mouse LPA -transfected1CHO cells is 0.025 and 0.023 M, respecti

18、vely.AM095 (free acid) is a potent LPA1 receptorantagonist with IC values of 0.98 and 0.73 M50for recombinant human or mouse LPA1 respectively.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.28%Clinical Data: No Development ReportedS

19、ize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/AM966.html AM966 HYPERLINK https:/www.MedChemE/AM966.html HYPERLINK https:/www.MedChemE/Amiselimod-hydrochloride.html Amiselimod HYPERLINK https:/www.MedChemE/Amiselimod-hydrochloride.html HYPERLINK https:/www.MedChemE

20、/Amiselimod-hydrochloride.html hydrochlorideCat. No.: HY-15277(MT-1303 hydrochloride) Cat. No.: HY-16734AAM966 is a high affinity, selective, oralLPA -antagonist, inhibits LPA-stimulated1intracellular calcium release (IC =17 nM).50Amiselimod hydrochloride is a novel sphingosine1-phosphate receptor-1

21、 (S1P1) modulator, designedto reduce the bradycardia effects associated withfingolimod and other S1P receptor modulators.Purity: 98.64%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.01%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 10

22、0 mg HYPERLINK https:/www.MedChemE/AS2717638.html AS2717638 HYPERLINK https:/www.MedChemE/AS2717638.html HYPERLINK https:/www.MedChemE/ASP-4058.html ASP-4058Cat. No.: HY-114379 Cat. No.: HY-111021AS2717638 is an oral active and selectivelysophosphatidic acid receptor 5 (LPA5)antagonist, with an IC o

23、f 38 nM for hLPA5.50AS2717638 also significantly improves PGE -,2PGF -, and AMPA-induced allodynia.2ASP-4058 is a next-generation, selective and oralbioactive agonist for Sphingosine 1-Phosphatereceptors 1 and 5 (S1P and S1P ), ameliorates1 5rodent experimental autoimmune encephalomyelitiswith a fav

24、orable safety profile.Purity: 99.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.43%Clinical Data: Phase 1Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/asp-4058-hydrochloride.html ASP-4

25、058 HYPERLINK https:/www.MedChemE/asp-4058-hydrochloride.html HYPERLINK https:/www.MedChemE/asp-4058-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/asp-4058-hydrochloride.html HYPERLINK https:/www.MedChemE/asp1126.html ASP1126Cat. No.: HY-111021A Cat. No.: HY-125881ASP-4058 hydrochlo

26、ride is a next-generation,selective and orally active agonist forSphingosine 1-Phosphate receptors 1 and 5 (S1P1and S1P ), ameliorates rodent experimental5autoimmune encephalomyelitis with a favorablesafety profile.ASP1126 is a selective and orally activesphingosine-1-phosphate (S1P) agonist, with E

27、C50values of 7.12 nM, 517 nM for hS1P and hS1P ,1 3respectively.Purity: 99.71%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/asp6432.html ASP6432 HYPERLINK https:/www.MedChem

28、E/asp6432.html HYPERLINK https:/www.MedChemE/BMS-986020.html BMS-986020Cat. No.: HY-120478 Cat. No.: HY-100619ASP6432 is a potent and selective type 1lysophosphatidic acid receptor (LPA1) antagonistwith IC s of 11 nM and 30 nM for human LPA1 and50rat LPA1, respectively.BMS-986020 is a high-affinity

29、and selectivelysophosphatidic acid receptor 1 (LPA1)antagonist. BMS-986020 inhibits bile acid andphospholipid transporters with IC s of 4.8 M,506.2 M, and 7.5 M for BSEP, MRP4, and MDR3,respectively.Purity: 95.50%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurit

30、y: 99.53%Clinical Data: Phase 2Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bms-986020-sodium.html BMS-986020 HYPERLINK https:/www.MedChemE/bms-986020-sodium.html HYPERLINK https:/www.MedChemE/bms-986020-sodium.html sodium HYPERLINK https:/www.MedChemE/bms-986020-

31、sodium.html HYPERLINK https:/www.MedChemE/bms-986278.html BMS-986278Cat. No.: HY-100619A Cat. No.: HY-139853BMS-986020 sodium is a high-affinitylysophosphatidic acid receptor 1 (LPA1)antagonist. BMS-986020 sodium inhibits bile acidand phospholipid transporters with IC s of 4.850M, 6.2 M, and 7.5 M f

32、or BSEP, MRP4, and MDR3,respectively.BMS-986278 is a potent lysophosphatidic acidreceptor 1 (LPA1) antagonist, with a human LPA1Kb of 6.9 nM.Purity: 99.60%Clinical Data: Phase 2Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.08%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25

33、 mg, 50 mg HYPERLINK https:/www.MedChemE/cay10444.html CAY10444 HYPERLINK https:/www.MedChemE/cay10444.html HYPERLINK https:/www.MedChemE/Cenerimod.html Cenerimod(BML-241) Cat. No.: HY-119401 (ACT-334441) Cat. No.: HY-17606CAY10444 (BML-241) is a sphingosine-1-phosphate 3(S1P3) antagonist. CAY10444

34、inhibits by 37%S1P-induced increases in Ca2+ in HeLacells expressing S1P3 receptors.Cenerimod (ACT-334441) is a potent, selective andorally active S1P1 receptor modulator, with anEC of 1 nM. Cenerimod shows more than 36fold50selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, andhS1P5 receptor subtypes (

35、EC s=10000, 228,502134, and 36 nM, respectively).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.02%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Ceralifimod.html Ceralifimod HYPERLINK https:/www.MedChemE/Cer

36、alifimod.html HYPERLINK https:/www.MedChemE/ceranib-2.html Ceranib-2(ONO-4641) Cat. No.: HY-12685Cat. No.: HY-116147Ceralifimod (ONO-4641) is selective, high potentagonist for sphingosine 1-phosphate receptors 1and 5, with EC s of 27.3, 334 pM for human S1P50receptor 1 and 5, respectively.Ceranib-2

37、is a potent and nonlipid ceramidaseinhibitor that inhibits cellular ceramidaseactivity with an IC of 28 M in SKOV3 cells.50Purity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mgPurity: 99.25%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.M

38、edChemE/cs-2100.html CS-2100 HYPERLINK https:/www.MedChemE/cs-2100.html HYPERLINK https:/www.MedChemE/cym-5478.html CYM-5478Cat. No.: HY-108493 Cat. No.: HY-111253CS-2100 (Compound 10b) is a potent, selective,orally active and S1P3-sparing S1P1 agonist withan EC of 4.0 nM for human S1P . CS-2100 sho

39、ws50 1in vivo immunosuppressive efficacy in rats with anID (infective dose) of 0.407 mg/kg for HvGR.50CYM-5478 is a potent and highly selective S1P2agonist with an EC of 119nM in a50TGF-shedding assay. CYM-5478 protectsneural-derived cell lines against Cisplatintoxicity.Purity: 98%Clinical Data: No

40、Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cym-5482.html CYM-5482 HYPERLINK https:/www.MedChemE/cym-5482.html HYPERLINK https:/www.MedChemE/cym-5520.html CYM-5520Cat. No.: HY-111292 Cat. No.: HY-100953CYM-5482 i

41、s a potent and selective agonistSphingosine 1-phosphate receptor 2 (S1PR2) withan IC and of 1.0 and 1.03 M. CYM-548250 EC50has the potential for the research of cancerdiseases.CYM-5520 is a selective and allosteric sphingosine1-phosphate receptor 2 (S1PR2) agonist with anEC of 480 nM. CYM-5520 does

42、not activate50S1PR1, S1PR3, S1PR4 and S1PR5 receptors. CYM-5520can co-bind in the S1PR2 receptor with S1P.CYM-5520 can be used for osteoporosis research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg,

43、 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CYM-5541.html CYM-5541(ML249) Cat. No.: HY-101419 HYPERLINK https:/www.MedChemE/cym50179.html CYM50179Cat. No.: HY-116146CYM-5541 (ML249) is an selective and allostericS1P3 receptor agonist with an EC50 between 72and 132 nM.CYM50179 (compound 22n)

44、is a potent and selectiveS1P4-R (Sphingosine-1-phosphate4 receptor)agonist with an EC of 46 nM.50Purity: 98.0%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/cym50

45、260.html CYM50260 HYPERLINK https:/www.MedChemE/cym50260.html HYPERLINK https:/www.MedChemE/cym50308.html CYM50308Cat. No.: HY-108494(ML248) Cat. No.: HY-108495CYM50260 is a potent and exquisitely selectivesphingosine-1-phosphate 4 receptor (S1P -R)4agonist with an EC of 45 nM. CYM50260 displays50no

46、 activity against S1P -R, S1P -R, S1P -R and1 2 3S1P -R.5CYM50308 (ML248) is a potent, selective and highaffinity sphingosine-1-phosphate receptor 4(S1P4-R) agonist with an EC50 of 56 nM.CYM50308 displays 37-fold more selective forS1P -R than S1P -R.4 5Purity: 99.0%Clinical Data: No Development Repo

47、rtedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cym50358.html CYM50358 HYPERLINK https:/www.MedChemE/cym50358.html HYPERLINK https:/www.MedChemE/cym5442.html CYM5442Cat. No.: HY-136462 Cat. No

48、.: HY-10968CYM50358 is a potent and selective S1PR4antagonist, with an IC of 25 nM. CYM50358 can be50used for the research of influenza infection.CYM5442 is a potent, highly-selective and orallyactive sphingosine 1-phosphate (S1P1) receptoragonist with an EC of 1.35 nM. CYM5442 is50inactive against

49、S1P2, S1P3, S1P4, and S1P5.CYM5442 activates S1P1-dependent p42/p44-MAPKphosphorylation.Purity: 98.04%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.83%Clinical Data: No Development ReportedSize: 5 mg, 10 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMe

50、dChemE HYPERLINK https:/www.MedChemE/cym5442-hydrochloride.html CYM5442 HYPERLINK https:/www.MedChemE/cym5442-hydrochloride.html HYPERLINK https:/www.MedChemE/cym5442-hydrochloride.html hydrochlorideCat. No.: HY-10968A HYPERLINK https:/www.MedChemE/Etrasimod.html Etrasimod(APD334) Cat. No.: HY-12789

51、CYM5442 hydrochloride is a potent,highly-selective and orally active sphingosine1-phosphate (S1P1) receptor agonist with anEC of 1.35 nM. CYM5442 hydrochloride is50inactive against S1P2, S1P3, S1P4, and S1P5.Etrasimod (APD334) is a potent, selective andorally available antagonist of thesphingosine-1

52、-phosphate-1 (S1P ) receptor with1an IC value of 1.88 nM in CHO cells.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.82%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/fingolimod.html Fingolimod(FTY720 free base) Cat. No.: HY-11063 HYP

53、ERLINK https:/www.MedChemE/Fingolimod-hydrochloride.html Fingolimod HYPERLINK https:/www.MedChemE/Fingolimod-hydrochloride.html HYPERLINK https:/www.MedChemE/Fingolimod-hydrochloride.html hydrochloride(FTY720) Cat. No.: HY-12005Fingolimod (FTY720 free base) is a sphingosine1-phosphate (S1P) antagoni

54、st with an IC of500.033 nM in K562 and NK cells. Fingolimod also isa pak1 activator, a immunosuppressant.Fingolimod hydrochloride (FTY720), an analog ofsphingosine, is a potent sphingosine 1-phosphate(S1P) receptors modulator. Fingolimodhydrochloride is phosphorylated by sphingosinekinases, particul

55、arly by SK2, and then bindsS1PR1, 3, 4, and 5.Purity: 99.56%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mg, 1 g, 5 gPurity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/fingolimod-d4.html Fingolimod-d4(FTY720 free base

56、d-d4) Cat. No.: HY-11063S HYPERLINK https:/www.MedChemE/fingolimod-d4-hydrochloride.html Fingolimod-d4 HYPERLINK https:/www.MedChemE/fingolimod-d4-hydrochloride.html HYPERLINK https:/www.MedChemE/fingolimod-d4-hydrochloride.html hydrochloride(FTY720-d4) Cat. No.: HY-11063S1Fingolimod-d4 (FTY720 free

57、 based-d4) is thedeuterium labeled Fingolimod. Fingolimod (FTY720free base) is a sphingosine 1-phosphate (S1P)antagonist with an IC of 0.033 nM in K562 and NK50cells. Fingolimod also is a pak1 activator, aimmunosuppressant.Fingolimod-d4 hydrochloride (FTY720-d4) is thedeuterium labeled Fingolimod hy

58、drochloride.Fingolimod hydrochloride (FTY720) is a sphingosine1-phosphate (S1P) antagonist with an IC of500.033 nM in K562 and NK cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/w

59、ww.MedChemE/FTY720_S_-Phosphate.html FTY720 HYPERLINK https:/www.MedChemE/FTY720_S_-Phosphate.html HYPERLINK https:/www.MedChemE/FTY720_S_-Phosphate.html (S)-Phosphate HYPERLINK https:/www.MedChemE/FTY720_S_-Phosphate.html HYPERLINK https:/www.MedChemE/glpg2938.html GLPG2938(S)-FTY720P; (S)-FTY720 p

60、hosphate) Cat. No.: HY-15382Cat. No.: HY-139310FTY720 (S)-Phosphate is an agonist of S1Preceptor 1 (S1PR1), used in the research of acuteinflammatory diseases such as acute lung injury.GLPG2938 is a potent and selective S1P2antagonist. GLPG2938 can be used for the researchof idiopathic pulmonary fib