S1P Receptor
In vertebrates, S1P is found in the extracellular milieu and interacts with cell-surface receptors to regulate an array of cellular responses, including cell migration, differentiation and survival. S1P plays fundamental roles in morphogenetic mechanisms, such as collective cell migration, tissue inductive events and biomechanical signalling. S1P receptors exhibit unique as well as common G-proteincoupling properties. For example, S1P1 couples exclusively to the Gi/o family, whereas S1P2 is capable of coupling to Gi/o, to G12/13 as well as to the Gq family. This coupling results in the activation of small GTPases such as Rho, Rac and Ras. Further downstream effectors of S1P receptors include adenylate cylase, PI-3-kinase, phospholipase C, protein kinase C and intracellular calcium. S1P2 receptor activation results in Rho, Rho kinase and PTEN signalling, which disrupts adherens junctions. This receptor also inhibits cell migration induced by growth factors, such as platelet-derived growth factor (PDGF) and insulin-like growth factor (IGF), and chemokines, such as stromal-derived factor 1 (SDF1, CXCL12), C5a and CCL2. S1P signalling affects the collective behaviour of cells by regulating cell-matrix and cell-cell adhesion, as well as alterations to the cytoskeleton. As this signalling system is involved in human diseases, and given that therapeutic modulation of S1P receptors has just begun in the treatment of neuroinflammatory diseases, developmental insights may be useful in further application to human therapeutics.
References
1.Mendelson K,et al. Development. 2014;141(1):5–9.
References
1.Mendelson K,et al. Development. 2014;141(1):5–9.
GPCR/G Protein
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S1P Receptor
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Amgen-23
产品货号 : M35699
cas no: 1448706-15-7
Amgen-23 (compound 23) 是一种有效的鞘氨醇激酶 (SPHK) 抑制剂,对 SPHK1 和 SPHK2 的 IC50 分别为 20 nM 和 1.6 μM。Amgen-23 可用于抗癌研究。 -
Ozanimod hydrochloride
产品货号 : M35654
cas no: 1618636-37-5
Ozanimod (RPC-1063) hydrochloride 是一种鞘氨醇 1-磷酸 (S1P) 受体调节剂,可高亲和力地选择性结合 S1P 受体亚型 1 (S1P1) 和 S1P5 (S1P5)。Ozanimod hydrochloride 对 hS1P1和 hS1P5 受体具有调节作用,EC50 值分别为 1.03 nM 和 8.6 nM。Ozanimod hydrochloride 可用于复发性多发性硬化 (MS) 的研究。 -
W140 HBr
产品货号 : M35378
cas no: 1246817-25-3
W140 hydrobromide 是一种 S1P1 拮抗剂,Ki 值为 2.84 μM,可增强毛细血管渗漏,恢复淋巴细胞的分泌。 -
Vibozilimod
产品货号 : M35071
cas no: 1403232-33-6
Vibozilimod (SCD-044, example 33) 是 S1p1 受体的激动剂 (信息来自专利WO2012140020A1)。 -
AMG-369
产品货号 : M34499
cas no: 1202073-26-4
AMG-369 (AMG 247) is an S1P1/S1P5 dual agonist that delays the onset of experimental autoimmune encephalomyelitis in rats.