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CYM50374

Alias: CYM-50374 CYM 50374 CYM50374
CYM50374 is a novel and potent S1PR4 (Sphingosine-1-Phosphate receptor 4) antagonist.
CYM50374
CYM50374 Chemical Structure CAS No.: 1314212-81-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
1g
Other Sizes
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Product Description
CYM50374 is a novel and potent S1PR4 (Sphingosine-1-Phosphate receptor 4) antagonist.
CYM50374 is a novel and potent antagonist of the sphingosine-1-phosphate receptor 4, with an IC50 of 34 nM. It is a G protein-coupled receptor antagonist primarily expressed in hematopoietic and lymphatic tissues. The compound has a molecular weight of 341.42 and a molecular formula of C19H19NO3S. It is used as a research tool to study the role of S1P4 in immune cell trafficking and inflammatory responses.
Biological Activity I Assay Protocols (From Reference)
Targets
CYM50374 targets the S1P4 receptor, a G protein-coupled receptor involved in immune cell trafficking, lymphocyte egress, and inflammatory responses. It acts as a potent antagonist, blocking S1P4 signaling. This receptor is a member of the sphingosine-1-phosphate receptor family, which plays critical roles in the immune system.
ln Vitro
CYM50374 is a potent S1P4 antagonist with an IC50 of 34 nM. It selectively blocks S1P4 receptor signaling. The compound is used as a pharmacological tool to study the role of S1P4 in various biological processes, including immune cell trafficking and inflammation.
ln Vivo
In vivo activity data for CYM50374 is limited. As a potent and selective S1P4 antagonist, it is expected to modulate immune cell functions and inflammatory responses. The compound is used as a research tool to study the role of S1P4 in various disease models, including autoimmune and inflammatory conditions.
Enzyme Assay
CYM50374 is evaluated in cell-free receptor binding assays to determine its affinity and selectivity for S1P receptors. Radioligand binding displacement assays are performed using membrane preparations expressing S1P receptor subtypes. Competition binding experiments are conducted with increasing concentrations of CYM50374 and a fixed concentration of a labeled reference ligand.
Cell Assay
CYM50374 is assessed in cell-based functional assays to measure its antagonist activity at S1P4. Cells expressing S1P4 are treated with CYM50374, and receptor activity is measured by assessing downstream signaling pathways, such as GTPγS binding or calcium mobilization. IC50 values are determined to quantify the potency of receptor antagonism.
Animal Protocol
CYM50374 is administered in animal models to evaluate its effects on S1P4-mediated immune functions. However, specific animal study protocols are not extensively documented. The compound is typically formulated for in vivo administration using DMSO or other suitable vehicles.
ADME/Pharmacokinetics
CYM50374 has a molecular weight of 341.42 and a molecular formula of C19H19NO3S. It has a CAS number of 1314212-81-1. The compound should be stored as a powder at -20°C for long-term stability. It is soluble in DMSO.
Toxicity/Toxicokinetics
No detailed toxicity data is available for CYM50374. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized in the available literature.
References

[1]. Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3632-6.

Additional Infomation
CYM50374 is a novel and potent S1PR4 antagonist. It has a CAS number of 1314212-81-1. It is used as a pharmacological tool to study the role of S1P4 in immune cell trafficking, lymphocyte egress, and inflammatory responses. It is not approved for clinical use.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Exact Mass
341.1086
CAS #
1314212-81-1
Appearance
Typically exists as solid at room temperature
Chemical Name
5-(3-Methyl-thiophen-2-yl)-furan-2-carboxylic acid (4-hydroxymethyl-2,6-dimethyl-phenyl)-amide
Synonyms
CYM-50374 CYM 50374 CYM50374
HS Tariff Code
2934.99.9001
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)
Solubility Data
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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