S1P Receptor
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S7176 | SKI II | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S7177 | PF-543 | <1 mg/mL | 93 mg/mL | 93 mg/mL |
| S7174 | Opaganib (ABC294640) | <1 mg/mL | 76 mg/mL | 28 mg/mL |
| S5002 | Fingolimod (FTY720) HCl | 69 mg/mL | 69 mg/mL | 69 mg/mL |
| S7182 | JTE 013 | <1 mg/mL | 81 mg/mL | 34 mg/mL |
| S5950 | Fingolimod | <1 mg/mL | 13 mg/mL | 5 mg/mL |
| S7952 | Ozanimod (RPC1063) | <1 mg/mL | 81 mg/mL | 10 mg/mL |
| S8241 | Ponesimod | <1 mg/mL | 92 mg/mL | 92 mg/mL |
| S7179 | Siponimod (BAF312) | <1 mg/mL | 100 mg/mL | 44 mg/mL |
特异性亚型抑制剂
S1P Receptor产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7176 |
SKI IISKI 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。 |
D, representative merged IF images with DAPI nuclei staining (blue) in untreated (“Ctl”) and CoCl2-treated cells without (“Veh”), and with SKI-II co-treatment. Scale bar = 30 μm. N=5 independent samples per group. oligodendrocytes(defined by MBP immunoreactivity, red), oligodendrocyte progenitor cell(defined by NG2 immunoreactivity, green).
|
|
| S7177 |
PF-543PF-543是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，Ki为3.6 nM。 |
(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).
|
|
| 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。 |
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) HClFingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。 |
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 013JTE-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。 |
||
| S5950New |
FingolimodFingolimod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 |
PonesimodPonesimod(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。 |
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 IISKI 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。 |
D, representative merged IF images with DAPI nuclei staining (blue) in untreated (“Ctl”) and CoCl2-treated cells without (“Veh”), and with SKI-II co-treatment. Scale bar = 30 μm. N=5 independent samples per group. oligodendrocytes(defined by MBP immunoreactivity, red), oligodendrocyte progenitor cell(defined by NG2 immunoreactivity, green).
|
|
| S7177 |
PF-543PF-543是一种新型Sphingosine kinase 1 (SphK1， SK1) （鞘氨醇激酶）抑制剂，Ki为3.6 nM。 |
(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).
|
|
| 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。 |
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) HClFingolimod (FTY720) HCl是一种S1P拮抗剂，在K562 和 NK细胞中IC50为0.33 nM。 |
2012, 119(9):2176-7 2014, 76(3):325-37 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 013JTE-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 |
|---|---|---|---|
| S5950New |
FingolimodFingolimod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 |
PonesimodPonesimod(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。 |
2018, 32(1):214-223 |
Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.
|
