Lysophospholipid Receptor
Lysophospholipids (LPs) such as lysophosphatidic acid (LPA) and sphingosine 1-phosphate (S1P) are a class of bioactive lipids, which have a phosphate head group and a single fatty acyl chain attached to a 3-carbon backbone in their chemical structures. LPA and S1P are the best studied LPs and play pivotal roles in physiological events including cell proliferation, survival, motility, cytoskeletal changes, and electrophysiological changes as well as pathophysiological processes that include autoimmune disease, fibrotic disease, cancer, inflammation, bone diseases, pain, metabolic syndrome, infertility, and hair loss. LPs exert their effects by binding to specific G protein-coupled receptors (GPCRs) that are the largest membrane receptor family in the human genome and contain nearly 800 receptors (including olfactory receptors). There are currently six LPA (LPA1–6) and five S1P receptors (S1P1–5).
References
1.Kihara Y,et al. Exp Cell Res. 2015;333(2):171–177.
References
1.Kihara Y,et al. Exp Cell Res. 2015;333(2):171–177.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
Lysophospholipid Receptor
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Amiselimod hydrochloride
catalog no : M16743
cas no: 942398-84-7
A novel prodrug S1P receptor modulator lacking S1P3 receptor agonism to avoid bradycardia associated with fingolimod and other S1P receptor modulators. -
Ceralifimod
catalog no : M16432
cas no: 891859-12-4
A next-generation S1P receptor agonist selective for S1P1 and S1P5 with EC50 of 0.0273 nM and 0.334 nM. -
Ponesimod
catalog no : M16202
cas no: 854107-55-4
A potent, selective, orally active S1P1 receptor agonist with EC50 of 9.1 nM; shows weak activity on S1P3 (EC50=123 nM). -
CS-0777
catalog no : M16073
cas no: 827344-05-8
A potent, selective, orally active S1P receptor-1 (S1P1) agonist with EC50 of 1.1 nM, 320-fold selectivity over S1P3. -
Mocravimod
catalog no : M14745
cas no: 509092-16-4
A synthetic immunosuppressant that functions as a S1P1 receptor agonist.