1. GPCR/G Protein
  2. LPL Receptor
  3. CYM-5478

CYM-5478 

Cat. No.: HY-111253
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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.

For research use only. We do not sell to patients.

CYM-5478 Chemical Structure

CYM-5478 Chemical Structure

CAS No. : 870762-83-7

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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].

IC50 & Target[1]

S1PR2

119 nM (EC50)

S1PR1

1690 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

388.38

Formula

C₂₁H₁₉F₃N₂O₂

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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CYM-5478
Cat. No.:
HY-111253
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