1094042-01-9
1094042-01-9 structure
- Name: CYM5442
- Chemical Name: 2-[[4-[5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl]-2,3-dihydro-1H-inden-1-yl]amino]ethanol
- CAS Number: 1094042-01-9
- Molecular Formula: C23H27N3O4
- Molecular Weight: 409.47800
- Catalog: Signaling Pathways GPCR/G Protein LPL Receptor
- Create Date: 2016-03-05 01:59:29
- Modify Date: 2024-01-02 19:13:11
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CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS)[1][2].
| Name | 2-[[4-[5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl]-2,3-dihydro-1H-inden-1-yl]amino]ethanol |
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| Synonyms |
CYM-5442
2-(4-(5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl amino) ethanol 2-(4-(5-(3,4-Diethoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-ylamino)ethanolhydrochloride CYM5442 |
| Description | CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS)[1][2]. |
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| Related Catalog | |
| Target |
EC50: 1.35 nM (Sphingosine 1-phosphate (S1P1) receptor)[1] |
| In Vitro | CYM5442 (0.5 µM; 0-60 minutes; HEK293 cells) treatment stimulates S1P1 phosphorylation in a time-dependent manner in P32-orthophosphate labeled cells[1]. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation in CHO-K1 cells transfected with S1P1 with an EC50 of 46 nM. The R120 for alanine (R120A) mutant is still able to maintain p42/p44-MAPK activity when incubated with CYM5442 (EC50 of 67 nM). Activation of p42/p44-MAPK by CYM5442 in E121A S1P1 cells is concentration dependent, with a mean EC50 value of 134 nM[1]. Western Blot Analysis[1] Cell Line: HEK293 cells stably expressing S1P1 fused to GFP on the carboxy-terminus Concentration: 0.5 µM Incubation Time: 0 minutes, 2 minutes, 5 minutes, 10 minutes, 30 minutes, 60 minutes Result: Stimulated S1P1 phosphorylation in a time-dependent manner. |
| In Vivo | CYM5442 (1 mg/kg; intraperitoneal injection; daily; for 5 days; adult male albino Wistar rats) treatment shows preserved visual function of visual evoked potentials (VEP). Retinal nerve fiber layer (RNFL) is significantly thicker in the CYM treated-animals compared to the vehicle[2]. Animal Model: Adult male albino Wistar rats (8-10 weeks old; 180-230 g) infected ocular endothelin-1 (ET-1)[2] Dosage: 1 mg/kg Administration: Intraperitoneal injection; daily; for 5 days Result: Visual evoked potentials (VEP) showed preserved visual function. Showed significantly higher retinal ganglion cells (RGCs) numbers. |
| References |
| Molecular Formula | C23H27N3O4 |
|---|---|
| Molecular Weight | 409.47800 |
| Exact Mass | 409.20000 |
| PSA | 89.64000 |
| LogP | 4.16110 |
| Storage condition | -20℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| RIDADR | NONH for all modes of transport |
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1094042-01-9 |
| Literature: WO2009/151529 A1, ; Page/Page column 150 ; WO 2009/151529 A1 |
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1094042-01-9 |
| Literature: WO2009/151529 A1, ; WO 2009/151529 A1 |
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1094042-01-9 |
| Literature: WO2009/151529 A1, ; WO 2009/151529 A1 |
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1094042-01-9 |
| Literature: WO2009/151529 A1, ; WO 2009/151529 A1 |
| Precursor 4 | |
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| DownStream 0 | |