S1P Receptor

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

S1P Receptor产品

所有产品 S1P Receptor抑制剂(4) S1P Receptor拮抗剂(2) S1P Receptor调节剂(4) 新S1P Receptor产品

产品目录	产品描述	文献引用	实验数据
S7176	SKI II SKI II是一种高度选择性的，非ATP竞争性的sphingosine kinase (SphK)抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。	Neurochem Int, 2016, 94:90-7 Cancer Chemother Pharmacol, 2014, 73(1):69-77 Int J Mol Med, 2017, 39(5):1277-1284	Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.
S7177	PF-543 PF-543是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，K_i为3.6 nM。	Int J Biochem Cell Biol, 2017, 90:17-28 Biochem Biophys Res Commun, 2016, 470(3):728-34	(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; P < 0.05, *P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
S6418^New	PF 429242 PF 429242是S1P抑制剂，IC50为170 nM。在其浓度高达100 μM时，PF 429242对胰蛋白酶、弹性蛋白酶、蛋白酶K、胞浆素、激肽释放酶、factor XIa、凝血酶或弗林蛋白酶没有显著抑制作用，而对尿激酶和factor Xa仅具有中等抑制作用。
S7174	Opaganib (ABC294640) Opaganib (ABC294640)是一种口服生物可利用的选择性sphingosine kinase-2 (SphK2)抑制剂，IC50约为 60 μM。Phase 1/2。	Inflammation, 2018, 41(4):1498-1507	Macrophages treated with ABC294640 at concentrations of 0, 0.5, 1, 5, 10, 50, or 100 nM. Ratios of OD/OD (NC) are presented as means ± standard deviation. *p < 0.05 vs. NC group (1‰ DMSO).
S5002	Fingolimod (FTY720) HCl Fingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。	Blood, 2012, 119(9):2176-7 Ann Neurol, 2014, 76(3):325-37 Leukemia, 2015, 29(4):847-57	Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6 105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8).
S7182	JTE 013 JTE-013是sphingosine 1-phosphate receptor 2(S1P2)拮抗剂（IC50=17.6 nM）。在超过10 μM的浓度下，对S1P1或S1P3没有作用。在HTC4细胞中，JTE-013拮抗S1P4的Ki值为237 nM。
S5950^New	Fingolimod Fingolimod是S1PR调节剂，用于治疗缓解型多发性硬化症。
S7952	Ozanimod (RPC1063) Ozanimod (RPC1063)是一种选择性口服的 S1P Receptor 1 调节剂。Phase 3。
S8241	Ponesimod Ponesimod(ACT-128800)是一种具有口服活性的S1P1免疫调制剂，其EC50为5.7 nM。
S7179	Siponimod (BAF312) BAF312 (Siponimod)是一种二代S1P受体调节剂，选择性作用于S1P1和S1P5受体，EC50分别为0.39 nM和0.98 nM，比作用于S1P2， S1P3和S1P4受体选择性高1000倍以上。 Phase 3。	Leukemia, 2018, 32(1):214-223	Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.

产品目录	产品描述	文献引用	实验数据
S7176	SKI II SKI II是一种高度选择性的，非ATP竞争性的sphingosine kinase (SphK)抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。	Neurochem Int,2016, 94:90-7 Cancer Chemother Pharmacol,2014, 73(1):69-77 Int J Mol Med,2017, 39(5):1277-1284	Transwell migration and invasion assays were performed. The stained cells were counted in five random fields at ×200 magnification, and the average number was taken. The average number of Control group (cells transduced with pLVX and treated with DMSO) was set as 100%, and relative migration and invasion of other groups was calculated by comparison of the cell number with the average number of control group. ***P < 0.001 versus pLVX + DMSO; ###P < 0.001 versus pLVX-p53 + DMSO.
S7177	PF-543 PF-543是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，K_i为3.6 nM。	Int J Biochem Cell Biol,2017, 90:17-28 Biochem Biophys Res Commun,2016, 470(3):728-34	(C) Western blot analysis of mature TGF-β1, FN and Col-I protein levels in sham, sham+ PF-543, UUO and UUO +PF-543 groups at 7 days (n =3). (average ± SEM; ANOVA; P < 0.05, *P < 0.01 versus sham group. #P < 0.05 versus UUO group). (D) Periodic acid-Schiff staning showed that tubular atrophy was evident in the obstructed kidneys at UUO 7 days after PF-543 treatment (n =6). (E) Masson's trichrome staining showed that matrix accumulation increased in the obstructed kidneys at UUO 7 days after PF-543 treatment(n = 6). (original magnification, ×400, scale bar =50 μm).
S6418^New	PF 429242 PF 429242是S1P抑制剂，IC50为170 nM。在其浓度高达100 μM时，PF 429242对胰蛋白酶、弹性蛋白酶、蛋白酶K、胞浆素、激肽释放酶、factor XIa、凝血酶或弗林蛋白酶没有显著抑制作用，而对尿激酶和factor Xa仅具有中等抑制作用。
S7174	Opaganib (ABC294640) Opaganib (ABC294640)是一种口服生物可利用的选择性sphingosine kinase-2 (SphK2)抑制剂，IC50约为 60 μM。Phase 1/2。	Inflammation,2018, 41(4):1498-1507	Macrophages treated with ABC294640 at concentrations of 0, 0.5, 1, 5, 10, 50, or 100 nM. Ratios of OD/OD (NC) are presented as means ± standard deviation. *p < 0.05 vs. NC group (1‰ DMSO).

产品目录	产品描述	文献引用	实验数据
S5002	Fingolimod (FTY720) HCl Fingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。	Blood, 2012, 119(9):2176-7 Ann Neurol, 2014, 76(3):325-37 Leukemia, 2015, 29(4):847-57	Fingolimod blocks antitumor immunity and prevents rejection of myeloma and B-cell lymphoma in TCR-transgenic SCID mice. (A) Id-specific TCR-transgenic (TCR-tg) SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 myeloma cells and treated daily with either fingolimod (FTY720, Selleck Chemicals; 2ug/g bodyweight) or with vehicle only (0.8% DMSO; Sigma-Aldrich) delivered intraperitoneally. Tumor growth was followed by palpation. Mice were euthanized when the tumor reached 10 mm in diameter (n=14-17). (B) Id-specific TCR-transgenic SCID mice were inoculated subcutaneously with 1.6 105 F9 B-lymphoma cells and treated daily with fingolimod or with vehicle only. F9 cells are A20 B-lymphoma cells transfected with Id-containing L-chain from MOPC3157 (n=14-16). (C) Nontransgenic SCID mice were inoculated subcutaneously with 1.6 105 MOPC315 cells and treated daily with fingolimod or with vehicle only (n=8).
S7182	JTE 013 JTE-013是sphingosine 1-phosphate receptor 2(S1P2)拮抗剂（IC50=17.6 nM）。在超过10 μM的浓度下，对S1P1或S1P3没有作用。在HTC4细胞中，JTE-013拮抗S1P4的Ki值为237 nM。

产品目录

产品描述

文献引用

实验数据

S5002

Fingolimod (FTY720) HCl

Fingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。

Blood, 2012, 119(9):2176-7

Ann Neurol, 2014, 76(3):325-37

Leukemia, 2015, 29(4):847-57

S7182

JTE 013

JTE-013是sphingosine 1-phosphate receptor 2(S1P2)拮抗剂（IC50=17.6 nM）。在超过10 μM的浓度下，对S1P1或S1P3没有作用。在HTC4细胞中，JTE-013拮抗S1P4的Ki值为237 nM。

产品目录	产品描述	文献引用	实验数据
S5950^New	Fingolimod Fingolimod是S1PR调节剂，用于治疗缓解型多发性硬化症。
S7952	Ozanimod (RPC1063) Ozanimod (RPC1063)是一种选择性口服的 S1P Receptor 1 调节剂。Phase 3。
S8241	Ponesimod Ponesimod(ACT-128800)是一种具有口服活性的S1P1免疫调制剂，其EC50为5.7 nM。
S7179	Siponimod (BAF312) BAF312 (Siponimod)是一种二代S1P受体调节剂，选择性作用于S1P1和S1P5受体，EC50分别为0.39 nM和0.98 nM，比作用于S1P2， S1P3和S1P4受体选择性高1000倍以上。 Phase 3。	Leukemia, 2018, 32(1):214-223	Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.

研究领域

产品类型

S1P Receptor

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

S1P Receptor产品