CYM5442
Modify Date: 2024-01-02 19:13:11
CYM5442 structure
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Common Name | CYM5442 | ||
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| CAS Number | 1094042-01-9 | Molecular Weight | 409.47800 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H27N3O4 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of CYM5442CYM5442 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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| Synonym | More Synonyms |
| 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 |
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| 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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CYM5442 CAS#:1094042-01-9 |
| Literature: WO2009/151529 A1, ; Page/Page column 150 ; WO 2009/151529 A1 |
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CYM5442 CAS#:1094042-01-9 |
| Literature: WO2009/151529 A1, ; WO 2009/151529 A1 |
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CYM5442 CAS#:1094042-01-9 |
| Literature: WO2009/151529 A1, ; WO 2009/151529 A1 |
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CYM5442 CAS#:1094042-01-9 |
| Literature: WO2009/151529 A1, ; WO 2009/151529 A1 |
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The spleen responds to intestinal manipulation but does not participate in the inflammatory response in a mouse model of postoperative ileus.
PLoS ONE 9(7) , e102211, (2014) Postoperative ileus is characterized by a transient impairment of the gastrointestinal motility after abdominal surgery. The intestinal inflammation, triggered by handling of the intestine, is the mai... |
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Sphingosine-1-Phosphate/Sphingosine-1-Phosphate Receptor 2 Axis Can Promote Mouse and Human Primary Mast Cell Angiogenic Potential through Upregulation of Vascular Endothelial Growth Factor-A and Matrix Metalloproteinase-2.
Mediators Inflamm. 2016 , 1503206, (2016) Mast cells (MC) are present in most vascularized tissues around the vasculature likely exerting immunomodulatory functions. Endowed with diverse mediators, resident MC represent first-line fine-tuners... |
| 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 |