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(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
Lysophospholipid Receptor
-
Amiselimod hydrochloride
产品货号 : M16743
cas no: 942398-84-7
一种新型前药 S1P 受体调节剂,缺乏 S1P3 受体激动作用,可避免与芬戈莫德和其他 S1P 受体调节剂相关的心动过缓。 -
Ceralifimod
产品货号 : M16432
cas no: 891859-12-4
下一代 S1P 受体激动剂,对 S1P1 和 S1P5 具有选择性,EC50 分别为 0.0273 nM 和 0.334 nM。 -
Ponesimod
产品货号 : M16202
cas no: 854107-55-4
一种有效的、选择性的、口服活性的 S1P1 受体激动剂,EC50 为 9.1 nM;对 S1P3 表现出弱活性 (EC50=123 nM)。 -
CS-0777
产品货号 : M16073
cas no: 827344-05-8
一种有效的、选择性的、口服活性的 S1P 受体-1 (S1P1) 激动剂,EC50 为 1.1 nM,选择性是 S1P3 的 320 倍。 -
Mocravimod
产品货号 : M14745
cas no: 509092-16-4
一种合成免疫抑制剂,具有 S1P1 受体激动剂的作用。