TCJL37 

TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a K_i of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD)^[1].

In cell-based assays, TCJL37 (Compound 37) shows IL-12 pSTAT4 EC₅₀ of 224 nM. TCJL37 shows EC₅₀s of 168 nM and 737 nM In human peripheral blood mononuclear cells (PBMC) and human whole blood assay, respectively^[1].

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

TCJL37 exhibits excellent oral exposure in CD-1 mice following oral administration (100 mg/kg). TCJL37 exhibits low clearance (1.0 mL/min/kg) in rat^[1].

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

376.74

C₁₇H₁₁ClF₂N₄O₂

1258294-34-6

Solid

Light yellow to light brown

O=C(NC1=CC(NC([C@@H]2[C@H](F)C2)=O)=NC=C1)C3=C(F)C=C(C#N)C=C3Cl

Room temperature in continental US; may vary elsewhere.

* 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.

• [1]. Jun Liang, et al. Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36.  [Content Brief]