| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
TC-G1001 specifically targets the G protein-coupled receptor 35 (GPR35), an orphan receptor belonging to the rhodopsin-like GPCR family. The compound acts as a potent agonist at this receptor, exhibiting pEC50 values of 7.59 for β-arrestin recruitment assays and 8.36 for Gαq-i5 Ca²⁺ mobilization assays. GPR35 is activated by various endogenous ligands including kynurenic acid, a tryptophan metabolite, and plays important roles in pain perception, immune cell function, and gastrointestinal motility. TC-G1001 demonstrates remarkable species selectivity, being 1000-fold more potent at human GPR35 receptors relative to mouse and rat orthologs. This species specificity makes the compound particularly valuable for studying human GPR35 function in experimental systems.
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| ln Vitro |
In vitro, TC-G1001 exhibits potent agonist activity at human GPR35 receptors with pEC50 values of 7.59 for β-arrestin recruitment and 8.36 for Gαq-i5 Ca²⁺ mobilization assays. The compound demonstrates approximately 1000-fold greater potency at human GPR35 compared to mouse and rat GPR35 orthologs in IP1 accumulation assays, indicating pronounced species selectivity. In comparative studies, TC-G1001 is more effective than zaprinast, a prototypical GPR35 agonist, suggesting superior pharmacological properties. The compound's potent and selective agonist activity makes it suitable for studying GPR35-mediated signaling pathways, including Gαq/11-mediated phospholipase C activation and downstream calcium mobilization, as well as β-arrestin recruitment and receptor internalization.
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| ln Vivo |
In vivo activity of TC-G1001 has been investigated in preclinical models to elucidate the physiological and pathophysiological roles of GPR35. As a potent and selective GPR35 agonist, the compound is expected to modulate GPR35-dependent signaling pathways in vivo, affecting processes such as pain perception, immune responses, and gastrointestinal motility. The compound's high potency at human GPR35, combined with its significantly lower activity at rodent orthologs, makes it particularly valuable for studies using humanized mouse models or for in vitro investigations using human tissues. Specific in vivo efficacy data in disease models is limited in publicly available sources, as the compound is primarily used as a research tool for target validation and pathway dissection.
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| Enzyme Assay |
The binding affinity and functional activity of TC-G1001 at GPR35 are typically assessed using cell-based functional assays rather than direct binding assays. For β-arrestin recruitment assays, cells expressing human GPR35 are treated with varying concentrations of the compound, and β-arrestin recruitment is quantified using BRET or enzyme complementation technologies. For Gαq-i5 Ca²⁺ mobilization assays, cells expressing GPR35 and the chimeric Gαq-i5 protein are loaded with calcium-sensitive fluorescent dyes, and the increase in intracellular calcium following compound addition is measured using fluorometric imaging plate readers (FLIPR). IP1 accumulation assays measure the accumulation of inositol monophosphate (IP1) as a surrogate for phospholipase C activation. pEC50 values are calculated from concentration-response curves.
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| Cell Assay |
Cellular assays for TC-G1001 typically employ recombinant cell lines engineered to express human GPR35. For β-arrestin recruitment assays, cells are transfected with GPR35 and β-arrestin fusion proteins, then treated with varying concentrations of TC-G1001. For calcium mobilization assays, cells are loaded with calcium-sensitive fluorescent dyes such as Fluo-4 or Fura-2, and the fluorescence signal is monitored in real-time following compound addition using FLIPR or similar plate readers. IP1 accumulation assays involve treating cells with the compound in the presence of lithium chloride to inhibit IP1 degradation, followed by quantification of accumulated IP1 using HTRF or ELISA-based detection. The compound's species selectivity can be confirmed by comparing activity at human versus mouse and rat GPR35 orthologs in parallel assays.
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| Animal Protocol |
In vivo studies with TC-G1001 are typically conducted in rodent models to investigate GPR35 function, though the compound's 1000-fold selectivity for human over rodent GPR35 presents challenges for interpreting results in standard mouse and rat models. For studies requiring in vivo GPR35 activation, researchers may use humanized transgenic mice expressing human GPR35 or employ alternative species with greater receptor homology. The compound is typically formulated in suitable vehicles such as DMSO, PEG300, or saline-based solutions for administration via intraperitoneal (i.p.) injection or oral gavage. Pharmacodynamic endpoints may include assessment of pain responses, gastrointestinal motility, immune cell activation, or other GPR35-regulated physiological processes.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TC-G1001 (molecular weight 342.34, molecular formula C17H11FN2O3S) have been partially characterized. The compound has a calculated LogP of 3.5, indicating moderate lipophilicity that may influence its absorption and distribution characteristics. For in vitro use, TC-G1001 is soluble in DMSO, allowing preparation of stock solutions for cellular assays. Storage recommendations include powder storage at -20°C for up to 3 years and solution storage at -80°C for 6 months or -20°C for 1 month, with protection from light during transport and storage. The compound is stable at ambient temperature for several days during shipping. Comprehensive PK parameters including oral bioavailability, half-life, and volume of distribution have not been detailed in publicly available sources.
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| Toxicity/Toxicokinetics |
TC-G1001 is intended for research use only and is not approved for human therapeutic applications. Comprehensive toxicological evaluations, including acute and repeat-dose toxicity studies in animal models, have not been reported in publicly available sources. The compound's high selectivity for human GPR35 suggests that off-target effects may be limited, but standard safety pharmacology assessments would be required if the compound were to be considered for therapeutic development. Researchers should handle the compound with appropriate safety precautions, including the use of personal protective equipment and proper laboratory practices for handling research chemicals.
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| References |
1. Neetoo-Isseljee et al (2013) High-throughput identification and characterization of novel, species-selective GPR35 agonists. J.Pharmacol.Exp.Ther. 344 568 PMID: 23262279
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| Additional Infomation |
TC-G1001 is a research-grade compound used as a pharmacological tool for studying GPR35 biology and signaling. GPR35 is an orphan GPCR that has emerged as a potential therapeutic target for pain, inflammatory diseases, and gastrointestinal disorders. The compound's remarkable species selectivity (1000-fold greater potency at human versus rodent GPR35) makes it a unique tool for studying human GPR35 function, though this property also limits its utility in standard rodent models. TC-G1001 is more potent than zaprinast, a previously used GPR35 agonist, and serves as a valuable reference compound for characterizing GPR35-mediated signaling pathways. The compound is available with purity specifications and is used in academic and pharmaceutical research settings for target validation and drug discovery applications.
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| Molecular Formula |
C17H11FN2O3S
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| Molecular Weight |
342.34
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| Exact Mass |
342.047
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| Elemental Analysis |
C, 59.64; H, 3.24; F, 5.55; N, 8.18; O, 14.02; S, 9.36
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| CAS # |
494191-73-0
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| PubChem CID |
135468531
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| Appearance |
Off-white to pink solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
540.8±60.0 °C at 760 mmHg
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| Flash Point |
280.9±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.672
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| LogP |
3.5
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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 |
3
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| Heavy Atom Count |
24
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| Complexity |
570
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=CC=C1N=C2NC(/C(/S2)=C\C3=CC=C(C(O)=O)C=C3)=O
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| InChi Key |
SYCKPHBALHXMIR-NTEUORMPSA-N
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| InChi Code |
InChI=1S/C17H11FN2O3S/c18-12-3-1-2-4-13(12)19-17-20-15(21)14(24-17)9-10-5-7-11(8-6-10)16(22)23/h1-9H,(H,22,23)(H,19,20,21)/b14-9+
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| Chemical Name |
4-[[2-[(2-Fluorophenyl)amino]-4-oxo-5(4H)-thiazolylidene]methyl]benzoic acid
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| Synonyms |
TC-G 1001
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~25 mg/mL (~73.03 mM)
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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 | 2.9211 mL | 14.6054 mL | 29.2107 mL | |
| 5 mM | 0.5842 mL | 2.9211 mL | 5.8421 mL | |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9211 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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