2. GPCR/G Protein
  3. LPL Receptor
  4. CYM5442

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).

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CYM5442 Chemical Structure

CYM5442 Chemical Structure

CAS No. : 1094042-01-9

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Based on 1 publication(s) in Google Scholar

Other Forms of CYM5442:

CYM5442 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CYM5442

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  • Purity & Documentation

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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].

IC50 & 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].

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

CYM5442 Related Antibodies

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].

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

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.
Molecular Weight

409.48

Formula

C23H27N3O4
CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

CCOC1=CC=C(C2=NC(C3=CC=CC4=C3CCC4NCCO)=NO2)C=C1OCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2.63 mg/mL (6.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4421 mL 12.2106 mL 24.4212 mL
5 mM 0.4884 mL 2.4421 mL 4.8842 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.83%

COA (252 KB) RP-HPLC (213 KB) LCMS (271 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4421 mL 12.2106 mL 24.4212 mL 61.0530 mL
5 mM 0.4884 mL 2.4421 mL 4.8842 mL 12.2106 mL
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CYM5442 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CYM54421094042-01-9CYM 5442CYM-5442LPL ReceptorLysophospholipid ReceptorS1P1endothelin-1CNSinternalizationphosphorylationp42/p44ubiquitinationretinalganglionInhibitorinhibitorinhibit

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