| 产品描述: | CYM-5478 is a potent and highly selective S1P2 agonist with an EC50 of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity. |
| 靶点: |
S1PR2:119 nM (EC50); S1PR1:1690 nM (EC50); S1PR3:1950 nM (EC50); S1PR4:>10 μM (EC50); S1PR5:>10 μM (IC50) |
| 体外研究: |
CYM-5478 activates S1P2 with an EC50 of 119 nM, has less than 25% efficacy and shows 10-fold lower potency against the other S1P receptor subtypes (EC50 of 1690 nM, 1950 nM, >10 μM, >10 μM for S1P1, S1P3, S1P4, S1P5, respectively). CYM-5478 (1, 10, 100, 1000, 10000 nM) induces a statistically significant increase in the viability of C6 cells in a dose dependent manner at concentrations above 100 nM under nutrient-deprivation stress produced by serum-starvation. This effect was absent in the presence of 10% fetal bovine serum. CYM-5478 (10 μM) causes a statistically significant, 3-fold increase in the EC50 of Cisplatin-mediated reduction in the viability of C6 glioma cells. CYM-5478 also attenuated Cisplatin-induced caspase 3/7 activity. CYM-5478 (10 μM) causes significantly attenuated the increase of ROS in C6 cells exposed to Cisplatin (20 μM; for 24 hours). CYM-5478 (20 μM) protects neural cells but not breast cancer cells against Cisplatin toxicity (C6 glioma cells: EC50=4.54 μM; GT1-7: EC50=17 μM; SK-N-BE2: EC50=7.44 μM; CLU188: EC50=5.54 μM). |
| 体内研究: |
CYM-5478 (1 mg/kg/day; ip) protects against Cisplatin-mediated (3 mg/kg; i.p.; once a week for 3 week) ototoxicity in rats. CYM-5478 (20 μM) treatment results in near-complete protection from cisplatin-mediated loss of neuromast viability. CYM-5478 pr 웿 Ů ñ 샮㡽䇘睜⪰ޏࠃ |
| 参考文献: |
1. Deron R Herr, et al. Sphingosine 1-phosphate receptor 2 (S1P2) attenuates reactive oxygen species formation and inhibits cell death: implications for otoprotective therapy. Sci Rep. 2016 Apr 15;6:24541. 2. Wei Wang, et al. Sphingosine 1-Phosphate Re 웿 Ů ñ 샮㡽䇘睜⪰ޏࠃ 䇩睜 |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.575 ml |
12.874 ml |
25.748 ml |
| 5 mM |
0.515 ml |
2.575 ml |
5.15 ml |
| 10 mM |
0.257 ml |
1.287 ml |
2.575 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.515 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |