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CYM-5478 (CYM5478) is a novel and potent agonist for S1P2 (Sphingosine 1-phosphate receptor 2, EC50 = 119 nM in a TGFα-shedding assay). CYM 5478 can protect neural-derived cell lines against Cisplatin toxicity.
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| ln Vitro |
In comparison to the other S1P receptor subtypes (EC50 of 1690 nM, 1950 nM, >10 μM, >10 μM for S1P1, S1P3, S1P4, and S1P5, respectively), CYM-5478 activates S1P2 with an EC50 of 119 nM, has less than 25% efficacy, and exhibits ten-fold reduced potency[1]. When serum fasting promotes nutrient-deprivation stress, CYM-5478 (1, 10, 100, 1000, and 10,000 nM) increases C6 cell viability in a dose-dependent manner at concentrations above 100 nM. When 10% fetal bovine serum was present, this effect did not occur[1]. CYM-5478 (10 μM) considerably attenuates the increase of ROS in C6 cells exposed to Cisplatin (20 μM; for 24 hours), and it also induces a statistically significant, 3-fold increase in the EC50 of Cisplatin-mediated decrease [1]. When exposed to Cisplatin toxicity, brain cells are shielded by CYM-5478 (20 μM) but not breast cancer cells (EC50=4.54 μM for C6 glioma cells, 17 μM for GT1-7, 7.44 μM for SK-N-BE2, and 5.54 μM for CLU188)[2].
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| ln Vivo |
Rats exposed to Cisplatin-mediated ototoxicity (3 mg/kg; ip; once a week for three weeks) are protected against by CYM-5478 (1 mg/kg/day; ip)[2]. When CYM-5478 (20 μM) is administered, neuromast viability loss caused by cisplatin is almost completely prevented. CYM-5478 guards against ototoxicity-related loss of hair cell viability in a zebrafish model[2].
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| References |
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| Molecular Formula |
C21H19F3N2O2
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| Molecular Weight |
388.4
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| Exact Mass |
388.139
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| Elemental Analysis |
C, 64.94; H, 4.93; F, 14.67; N, 7.21; O, 8.24
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| CAS # |
870762-83-7
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| PubChem CID |
7802604
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
527.1±50.0 °C at 760 mmHg
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| Flash Point |
272.6±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.558
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| LogP |
3.82
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
665
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1C([H])=C([H])C(N(C=1[H])C([H])([H])C(C1C([H])=C(C([H])([H])[H])N(C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])C=1C([H])([H])[H])=O)=O)(F)F
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| InChi Key |
RGSGTUIDJXHTTO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19F3N2O2/c1-14-10-18(15(2)26(14)11-16-6-4-3-5-7-16)19(27)13-25-12-17(21(22,23)24)8-9-20(25)28/h3-10,12H,11,13H2,1-2H3
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| Chemical Name |
1-[2-(1-Benzyl-2,5-dimethylpyrrol-3-yl)-2-oxoethyl]-5-(trifluoromethyl)pyridin-2-one
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| Synonyms |
CYM5478 CYM 5478 CYM-5478
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5747 mL | 12.8733 mL | 25.7467 mL | |
| 5 mM | 0.5149 mL | 2.5747 mL | 5.1493 mL | |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5747 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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