| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
TCJL-37 targets tyrosine kinase 2 (TYK2), a member of the Janus kinase (JAK) family involved in cytokine signaling. TYK2 mediates signaling through receptors for IL-12, IL-23, and type I interferons. By inhibiting TYK2, TCJL-37 blocks downstream signaling pathways and reduces the production of inflammatory cytokines such as IFNγ.
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| ln Vitro |
TCJL37 (compound 37) displayed an IL-12 pSTAT4 EC50 of 224 nM in cell-based experiments. Human whole blood and peripheral blood mononuclear cells (PBMC) had TCJL37 EC50 values of 737 nM and 168 nM, respectively [1].
In vitro, TCJL-37 is a potent TYK2 inhibitor with a Ki of 1.6 nM. It shows some selectivity for TYK2 over JAK1, JAK2, and JAK3. The compound's activity is assessed by measuring TYK2 inhibition in enzyme assays and by assessing downstream signaling in cell-based systems. |
| ln Vivo |
When TCJL37 was given orally (100 mg/kg), CD-1 mice exhibited great oral exposure. Rats with TCJL37 show poor clearance (1.0 mL/min/kg) [1].
In vivo, TCJL-37 is orally bioavailable and inhibits IFNγ production in mice. It has potential applications in the study and treatment of inflammatory bowel diseases (IBD) and other TYK2-mediated inflammatory conditions. Its oral bioavailability makes it suitable for oral administration in preclinical studies. |
| Enzyme Assay |
In vitro enzyme assays for TCJL-37 measure its inhibition of TYK2 kinase activity. The kinase is incubated with its substrate and ATP in the presence of varying concentrations of the compound. Kinase activity is measured by quantifying substrate phosphorylation using radioactive or fluorescence-based methods. A Ki of 1.6 nM is determined from enzyme kinetics studies.
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| Cell Assay |
In vitro cell-based assays for TCJL-37 assess its effects on TYK2-mediated signaling in cells. Cells are treated with serial dilutions of the compound, and TYK2-dependent signaling pathways are measured by assessing STAT phosphorylation or cytokine production (e.g., IFNγ). Selectivity over JAK1, JAK2, and JAK3 is confirmed in parallel assays.
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| Animal Protocol |
In vivo animal models for TCJL-37 include mouse models of inflammatory bowel disease (IBD) and other inflammatory conditions. The compound is administered orally, and its effects on disease severity, inflammatory cytokine production, and immune cell infiltration are evaluated. Pharmacodynamic studies measure TYK2 inhibition and IFNγ production in target tissues.
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| ADME/Pharmacokinetics |
TCJL-37 has a molecular formula of C17H12ClF2N4O2 and a molecular weight of 378.75 g/mol. It is also known as 2-Chloro-4-cyano-6-fluoro-N-(2-((1r,2r)-2-fluorocyclopropanecarboxamido)pyridin-4-yl)benzamide. The compound has a purity of ≥98% and is soluble in DMSO. It is stored at appropriate temperatures for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of TCJL-37 is characterized in preclinical safety studies. As a TYK2 inhibitor, the compound may affect immune function and cytokine signaling. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TCJL-37 (TC JL 37) is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. It shows some selectivity for TYK2 over JAK1, JAK2, and JAK3. TCJL-37 inhibits IFNγ production in vivo in mice and can be used for the research of inflammatory bowel diseases (IBD). The compound is intended for laboratory research use only.
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| Molecular Formula |
C17H11CLF2N4O2
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| Molecular Weight |
376.744649171829
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| Exact Mass |
376.053
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| CAS # |
1258294-34-6
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| Related CAS # |
1258294-34-6;
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| PubChem CID |
56934550
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
2.2
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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 |
26
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| Complexity |
613
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1C=C(C#N)C=C(C=1C(NC1C=CN=C(C=1)NC([C@H]1C[C@H]1F)=O)=O)F
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| InChi Key |
NKALKXMQBFLGQI-CMPLNLGQSA-N
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| InChi Code |
InChI=1S/C17H11ClF2N4O2/c18-11-3-8(7-21)4-13(20)15(11)17(26)23-9-1-2-22-14(5-9)24-16(25)10-6-12(10)19/h1-5,10,12H,6H2,(H2,22,23,24,25,26)/t10-,12+/m0/s1
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| Chemical Name |
2-Chloro-4-cyano-6-fluoro-N-[2-[[[(1R,2R)-2-fluorocyclopropyl]carbonyl]amino]-4-pyridinyl]benzamide
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| Synonyms |
TCJL-37 TCJL 37 TCJL37 TC JL-37 TC JL 37 TC JL37
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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 | 2.6544 mL | 13.2718 mL | 26.5435 mL | |
| 5 mM | 0.5309 mL | 2.6544 mL | 5.3087 mL | |
| 10 mM | 0.2654 mL | 1.3272 mL | 2.6544 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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