LPL Receptor Lysophospholipid Receptor

LPL Receptor (Lysophospholipid Receptor) group are members of the G -coupled receptor family of integral membrane that are important for lipid signaling. In humans, there are eight LPL receptors, each encoded by a separate . These LPL receptor are also sometimes referred to as "Edg". LPL receptor ligands bind to and activate their cognate receptors located in the cell membrane. Depending on which , receptor, and cell type is involved, the activated receptor can have a range of effects on the cell. These include primary effects of inhibition of adenylyl cyclase and release of calcium from the endoplasmic reticulum, as well as secondary effects of preventingapoptosis and increasing cell proliferation. Type: LPAR1, LPAR2, LPAR3, LPAR4, LPAR5, LPAR6, S1PR1, S1PR2, S1PR3, S1PR4, S1PR5.

www.MedChemExpress.com 1 LPL Receptor Inhibitors & Modulators

AM095 AM095 free acid Cat. No.: HY-16039 Cat. No.: HY-16040

Bioactivity: AM095 is a selective LPA1 receptor antagonist. The IC50 for Bioactivity: AM095 (free acid) is a potent LPA1 receptor antagonist with IC values of 0.98 and 0.73 μM for recombinant human or mouse AM095 antagonism of LPA-induced calcium flux of human or mouse 50

LPA 1-transfected CHO cells is 0.025 and 0.023 μM, LPA1 respectively. respectively. Purity: 98.14% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

AM966 Amiselimod hydrochloride Cat. No.: HY-15277 (MT-1303 hydrochloride) Cat. No.: HY-16734A

Bioactivity: AM966 is a high affinity, selective, oral LPA1-antagonist, Bioactivity: Amiselimod hydrochloride is a novel sphingosine 1-phosphate inhibits LPA-stimulated intracellular calcium release ( receptor-1 (S1P1) modulator, designed to reduce the IC =17 nM). bradycardia effects associated with and other S1P 50 receptor modulators.

Purity: 98.75% Purity: 99.02% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

AS2717638 ASP-4058 Cat. No.: HY-114379 Cat. No.: HY-111021

Bioactivity: AS2717638 is an oral active receptor 5 Bioactivity: ASP-4058 is a next-generation, selective and oral bioactive

(LPA5) antagonist in rodents. AS2717638 also significantly agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 improves PGE -, PGF -, and AMPA-induced allodynia [1]. 2 2α and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile [1]. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg

ASP6432 BMS-986020 Cat. No.: HY-120478 (AM152) Cat. No.: HY-100619

Bioactivity: ASP6432 is a potent and selective type 1 lysophosphatidic Bioactivity: BMS-986020 is an LPA1 antagonist. target: LPA1 BMS-986020 is in Phase 2 clinical development for treating idiopathic acid receptor (LPA1) antagonist with IC50s of 11 nM and 30 nM pulmonary fibrosis. BMS-986020 selectively inhibits the LPA for human LPA1 and rat LPA1, respectively [1]. receptor, which is involved in binding of the signaling molecule lysophosphatidic acid, which in turn is involved in a… Purity: >98% Purity: 99.53% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Cenerimod Ceralifimod (ACT-334441) Cat. No.: HY-17606 (ONO-4641) Cat. No.: HY-12685

Bioactivity: Cenerimod (ACT-334441) is a potent and orally available Bioactivity: Ceralifimod (ONO-4641) is selective, high potent agonist for

sphingosine 1-phosphate 1 receptor ( S1P1) agonist extracted sphingosine 1-phosphate receptors 1 and 5, with EC50s of from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, 27.3, 334 pM for human S1P receptor 1 and 5, respectively. with an EC50 of 2.7 nM.

Purity: 98.43% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CYM-5541 Etrasimod (ML249) Cat. No.: HY-101419 (APD334) Cat. No.: HY-12789

Bioactivity: CYM-5541 (ML249) is an selective and allosteric S1P3 Bioactivity: Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 ( S1P1) receptor receptor agonist with an EC50 between 72 and 132 nM. with an IC50 value of 1.88 nM in CHO cells.

Purity: 98.0% Purity: 99.64% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Fingolimod Fingolimod hydrochloride (FTY720 free base) Cat. No.: HY-11063 (FTY720) Cat. No.: HY-12005

Bioactivity: Fingolimod is a sphingosine 1-phosphate ( S1P) antagonist Bioactivity: Fingolimod hydrochloride is a sphingosine 1-phosphate ( S1P)

with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is antagonist with an IC50 of 0.033 nM in K562 and NK cells. a pak1 activator. Fingolimod hydrochloride also is a pak1 activator.

Purity: 99.95% Purity: 99.76% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 100 mg, 200 mg, 1 g, 5 g

FTY720 (S)-Phosphate GSK2018682 ((S)-FTY720P; (S)-FTY720 phosphate) Cat. No.: HY-15382 Cat. No.: HY-19511

Bioactivity: FTY720 (S)-Phosphate is an agonist of S1P receptor 1 Bioactivity: GSK2018682 is an agonist for S1P1 and S1P5 receptor with

(S1PR1), used in the research of acute inflammatory diseases pEC50s of 7.7 and 7.2, respectively, and has no agonist such as acute lung injury. activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of .

Purity: 98.0% Purity: 98.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Ki16425 LPA1 antagonist 1 (Debio 0719) Cat. No.: HY-13285 Cat. No.: HY-18076

Bioactivity: Ki16425 (Debio 0719) is a subtype-selective, competitive Bioactivity: LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid

antagonist of the EDG-family receptors, LPA1 and LPA3 with receptor-1 (LPA1) antagonist with an IC50 of 25 nM. Kis of 0.34 μM and 0.93 μM, respectively.

Purity: 98.67% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg

LPA2 antagonist 1 ONO-7300243 Cat. No.: HY-18075 Cat. No.: HY-100882

Bioactivity: LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM. Bioactivity: ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 ( LPA1) antagonist with IC50 of 0.16 μM.

Purity: 98.85% Purity: 98.04% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 3

Ozanimod PF429242 dihydrochloride (RPC-1063) Cat. No.: HY-12288 Cat. No.: HY-13447A

Bioactivity: Ozanimod is a potent and selective S1P1 and S1P5 receptor Bioactivity: PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM. agonist with EC50s of 410±160 pM and 11±4.3 nM in [ 35S]-GTPγS binding, respectively.

Purity: 99.81% Purity: 98.76% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Ponesimod Radioprotectin-1 (ACT-128800) Cat. No.: HY-10569 Cat. No.: HY-114380

Bioactivity: Ponesimod(ACT-128800) is an orally active, selective Bioactivity: Radioprotectin-1 is a potent and specific nonlipid agonist of

sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator. lysophosphatidic acid receptor 2 (LPA2), with an EC50 value [1] of 25 nM for murine LPA 2 subtype .

Purity: 99.53% Purity: 99.44% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

S1p receptor agonist 1 S1P1 Agonist III Cat. No.: HY-101265 Cat. No.: HY-12835

Bioactivity: S1p receptor agonist 1 is an S1P receptor agonist extracted Bioactivity: S1P1 Agonist III is a potent and orally active S1P1 agonist from patent WO 2015039587 A1, compound example 2. with EC50 of 18 nM; no activity on S1P3.

Purity: 98.28% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg

S1PR1 modulator 1 S1PR1-MO-1 Cat. No.: HY-126145 Cat. No.: HY-U00366

Bioactivity: S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a Bioactivity: S1PR-MO-1 is the modulator of sphingosine-1-phosphate

pIC50 of 7.6, with >40- and >80-fold selectivity, over receptor, used for research of hyperproliferative, inflammatory diseases. the other S1PR isoforms S1PR2/3/4 [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 500 mg, 250 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

SAR-100842 Cat. No.: HY-100185 (BAF-312) Cat. No.: HY-12355

Bioactivity: SAR-100842 is a lysophaphatidic acid 1 ( LPA1/ Edg-2) Bioactivity: Siponimod (BAF-312) is a potent and selective receptor inhibitor. sphingosine-1-phosphate (S1P) receptor modulator. It is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and

S1P4 ( EC50s of 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively). Used to treat adult multiple sclerosis. Purity: 99.69% Purity: 98.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1 g

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

TY-52156 W146 Cat. No.: HY-19736 (W-146; W 146) Cat. No.: HY-101395

Bioactivity: TY-52156 is a potent and selective S1P3 receptor antagonist Bioactivity: W146 is a selective antagonist of sphingosine-1-phosphate [1] receptor 1 ( S1PR1) with an EC 50 value of 398 nM. with a Ki value of 110 nM .

Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 5