| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
TCS-3035 targets GPR35, a G protein-coupled receptor that is activated by various endogenous and synthetic ligands. It is a potent agonist of GPR35 with a pEC50 of 5.86. By activating GPR35, TCS-3035 modulates downstream signaling pathways, which may include Gαi/o and Gα12/13-mediated signaling. The receptor is involved in various physiological processes, including immune function and metabolism.
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| ln Vitro |
In vitro, TCS-3035 is a potent agonist of GPR35 with a pEC50 of 5.86. It activates GPR35-mediated signaling pathways in cell-based assays. The compound's potency and selectivity make it a valuable tool for studying GPR35 function. Specific details on assay conditions and downstream signaling pathways are not extensively provided in the available literature.
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| ln Vivo |
In vivo activity of TCS-3035 is not extensively detailed in the available literature. As a GPR35 agonist, it would be expected to modulate GPR35-mediated physiological processes. GPR35 has been implicated in various conditions, including inflammatory diseases and metabolic disorders. Specific in vivo efficacy data, including dosing regimens and animal models, are not provided.
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| Enzyme Assay |
In vitro receptor binding and functional assays for TCS-3035 involve measuring GPR35 activation. Cells expressing GPR35 are treated with varying concentrations of TCS-3035. Receptor activation is measured by assessing downstream signaling pathways, such as cAMP accumulation, calcium mobilization, or β-arrestin recruitment. pEC50 values are calculated from concentration-response curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing GPR35 are cultured and treated with TCS-3035 at various concentrations. Receptor activation is measured using appropriate assays (e.g., cAMP ELISA, calcium flux assays, or β-arrestin recruitment assays). Cell viability is assessed using standard assays. The compound's effects on downstream signaling and gene expression can also be studied.
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| Animal Protocol |
In vivo animal studies for TCS-3035 would typically use rodent models to assess GPR35-mediated effects. The compound is administered orally or intraperitoneally at doses determined from pharmacokinetic studies. Physiological parameters, such as inflammatory markers or metabolic endpoints, are measured. Specific protocols are not extensively documented in the available literature.
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| ADME/Pharmacokinetics |
TCS-3035 has a molecular formula of (Z)-2-(4-((2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid and a molecular weight of 279.27 g/mol. The compound is provided as a powder. Detailed solubility, stability, and storage conditions are not extensively provided in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicity data for TCS-3035 are not extensively provided in the available literature. As a GPR35 agonist, it would be expected to have a safety profile related to modulation of this receptor. The compound is for research use only and is not for human or clinical use. Standard toxicology assessments would be required for therapeutic development.
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| References | |
| Additional Infomation |
TCS-3035 is a small-molecule, synthetic agonist for the G protein-coupled receptor GPR35. It is also known as GPR35 agonist 4 or compound 10. It demonstrates high potency as a GPR35 agonist with a pEC50 of 5.86. Research has definitively confirmed this compound as an agonist of GPR35. It is used as a research tool to study GPR35 signaling and function. No approved therapeutic status is reported.
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| Molecular Formula |
C12H9NO5S
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|---|---|
| Molecular Weight |
279.26
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| Exact Mass |
279.02
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| CAS # |
871085-49-3
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| PubChem CID |
2295463
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| Appearance |
White to off-white solid powder
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| LogP |
1.802
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
426
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1/C=C\2/C(=O)NC(=O)S2)OCC(=O)O
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| InChi Key |
WXMCOLGPDOYHNK-UITAMQMPSA-N
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| InChi Code |
InChI=1S/C12H9NO5S/c14-10(15)6-18-8-3-1-7(2-4-8)5-9-11(16)13-12(17)19-9/h1-5H,6H2,(H,14,15)(H,13,16,17)/b9-5-
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| Chemical Name |
2-[4-[(Z)-(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]phenoxy]acetic acid
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| Synonyms |
TCS3035; TCS 3035; TCS-3035
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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 | 3.5809 mL | 17.9045 mL | 35.8089 mL | |
| 5 mM | 0.7162 mL | 3.5809 mL | 7.1618 mL | |
| 10 mM | 0.3581 mL | 1.7904 mL | 3.5809 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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