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CYM-5478
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CYM-5478图片
CAS NO:870762-83-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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].

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].

分子量

388.38

Formula

C21H19F3N2O2

CAS 号

870762-83-7

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.