| Bioactivity | Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis[1]. | ||||||||||||
| Invitro | Tyk2-IN-5 inhibits Jak1-3 with IC50 values of >2 μM and displays the Jak1-3 dependent cellular activities of >12.5 μM (IC50 values)[1]. | ||||||||||||
| In Vivo | Tyk2-IN-5 (5, 10 mg/kg; p.o.; twice daily for 20 days) shows highly efficacious in a rat adjuvant arthritis model[1].Tyk2-IN-5 (1, 10 mg/kg; p.o.; single) inhibits IL-12/IL-18 induced IFNγ production in a dose-dependent manner[1].Tyk2-IN-5 (10 mg/kg; p.o.; single) shows a high oral exposure and bioavailability (114%) in rat[1]. Animal Model: | ||||||||||||
| Name | Tyk2-IN-5 | ||||||||||||
| CAS | 1797432-62-2 | ||||||||||||
| Formula | C21H19FN8O2 | ||||||||||||
| Molar Mass | 434.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Liu C, et al. Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. |
Tyk2-IN-5
CAS: 1797432-62-2 F: C21H19FN8O2 W: 434.43
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.