CYM-5478 structure
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Common Name | CYM-5478 | ||
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CAS Number | 870762-83-7 | Molecular Weight | 388.38 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | 527.1±50.0 °C at 760 mmHg | |
Molecular Formula | C21H19F3N2O2 | Melting Point | N/A | |
MSDS | N/A | Flash Point | 272.6±30.1 °C |
Use of CYM-5478CYM-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[1][2]. |
Name | CYM 5478 |
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Synonym | More Synonyms |
Description | 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[1][2]. |
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Related Catalog | |
Target |
S1PR1:1690 nM (EC50) S1PR2:119 nM (EC50) S1PR3:1950 nM (EC50) S1PR4:>10 μM (EC50) S1PR5:>10 μM (IC50) |
In Vitro | 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)[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 EC50 of 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]. |
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]. |
References |
Density | 1.2±0.1 g/cm3 |
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Boiling Point | 527.1±50.0 °C at 760 mmHg |
Molecular Formula | C21H19F3N2O2 |
Molecular Weight | 388.38 |
Flash Point | 272.6±30.1 °C |
Exact Mass | 388.139862 |
LogP | 3.82 |
Vapour Pressure | 0.0±1.4 mmHg at 25°C |
Index of Refraction | 1.558 |
CYM 5478 |
2(1H)-Pyridinone, 1-[2-[2,5-dimethyl-1-(phenylmethyl)-1H-pyrrol-3-yl]-2-oxoethyl]-5-(trifluoromethyl)- |
1-[2-(1-Benzyl-2,5-dimethyl-1H-pyrrol-3-yl)-2-oxoethyl]-5-(trifluoromethyl)-2(1H)-pyridinone |
MFCD07342414 |