CYM-5478 是一种有效,高度选择性的S1P2激动剂,在TGFα-脱落试验中EC50为119 nM。CYM-5478 保护神经衍生细胞系免受顺铂 (Cisplatin) 毒性。
生物活性 | CYM-5478 is a potent and highly selectiveS1P2agonist with anEC50of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity[1][2]. |
IC50& Target[1] | S1PR1 1690 nM (EC50) | S1PR2 119 nM (EC50) | S1PR3 1950 nM (EC50) | S1PR4 >10 μM (EC50) | S1PR5 >10 μM (IC50) |
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体外研究 (In Vitro) | CYM-5478 activates S1P2with an EC50of 119 nM, has less than 25% efficacy and shows 10-fold lower potency against the other S1P receptor subtypes (EC50of 1690 nM, 1950 nM, >10 μM, >10 μM for S1P1, S1P3, S1P4, S1P5, respectively)[1]. 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[1]. CYM-5478 (10 μM) causes a statistically significant, 3-fold increase in the EC50of Cisplatin-mediated reduction in the viability of C6 glioma cells. CYM-5478 also attenuated Cisplatin-induced caspase 3/7 activity[1]. CYM-5478 (10 μM) causes significantly attenuated the increase of ROS in C6 cells exposed to Cisplatin (20 μM; for 24 hours)[1]. 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)[2].
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体内研究 (In Vivo) | 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[2]. CYM-5478 (20 μM) treatment results in near-complete protection from cisplatin-mediated loss of neuromast viability. CYM-5478 protects against loss of hair cell viability in a zebrafish model for ototoxicity[2].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |