| Bioactivity | BTK-IN-17 (compound 36R) is a selective and orally activeBTK inhibitor with an IC50 value of 13.7 nM. BTK-IN-17 decreases the expression of p-BTKY223 and p-PLCγ2Y1217. BTK-IN-17 shows anti-inflammatory effects[1]. |
| Target | IC50: 13.7 nM (BTK) |
| Invitro | BTK-IN-17 (compound 36R) shows hERG channel inhibition with an IC50 value of 8.6 µM[1].BTK-IN-17 (0-10000 nM) decreases the expression of p-BTKY223 and p-PLCγ2Y1217 in Ramos cells[1]. Western Blot Analysis[1] |
| In Vivo | BTK-IN-17 (1 mg/kg i.v.; 10 mg/kg p.o.) 显示口服给药后一小时血浆浓度迅速达到 125 nM，BTK 占有率达到 79%，BTK 占有率在 24 小时后保持约 62% 在大鼠中[1].BTK-IN-17 (10, 30, 50 mg/kg; p.o.; once daily for 10 days) 在大鼠中显示出良好的抗炎作用[1]。 |
| Name | BTK-IN-17 |
| Formula | C26H23N7O2 |
| Molar Mass | 465.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Fang X, et al. Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis. Eur J Med Chem. 2022 Nov 25;246:114940. |