BTK inhibitor 17
- CAS No.
- 1858206-76-4
- Chemical Name:
- BTK inhibitor 17
- Synonyms
- BTK inhibitor 17;7H-Pyrazolo[3,4-d]pyridazin-7-one, 4-amino-1,6-dihydro-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-3-(4-phenoxyphenyl)-;BTK inhibitor17,oral,BTK inhibitor 17,Btk,rheumatoid,Inhibitor,inhibit,Cys481,Bruton tyrosine kinase,arthritis,BTK inhibitor-17
- CBNumber:
- CB08186702
- Molecular Formula:
- C25H24N6O3
- Molecular Weight:
- 456.5
- MDL Number:
- MFCD34167515
- MOL File:
- 1858206-76-4.mol
BTK inhibitor 17 Chemical Properties,Uses,Production
Biological Activity
BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research[1]. BTK inhibitor 17 (compound 8) could covalently bind to Cys481 and formed an HB network with hinge key residues Met477, Glu475, and gatekeeper Thr474[1]. BTK inhibitor 17 (compound 8; 3-10 mg/kg; oral gavage; daily; for 28 days) treatment inhibits the significant progression of the disease and exhibits a clear dose-dependent reduction per paw clinical scores, and no significant body weight loss is observed for all different dosages[1].BTK inhibitor 17 (compound 8) shows >95% plasma protein binding across three species of human, rat, and mouse. After an intravenous injection, the half-life (rat, 0.32 h; mice, 0.42 h), clearance (rat, 54.6 mL/min/kg; mice, 31.3 mL/min/kg), volume of distribution (rat, 1.55 L/kg; mice, 0.82 L/kg), and AUC exposure (rat, 604 ng.h/mL; mice, 576 ng.h/mL) are observed in two species. After oral administration, BTK inhibitor 17 exhibits higher Cmax (rat, 466 ng/mL; mice, 252 ng/mL) and plasma exposure (rat, 642 ng.h/mL; mice, 128 ng.h/mL) with a favorable oral bioavailability (rat, 23.7%; mice, 11.2%)[1].
References
[1]. Xuejun Zhang, et al. Discovery and Evaluation of Pyrazolo[3,4- d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor. ACS Med Chem Lett. 2019 Dec 11;11(10):1863-1868.
BTK inhibitor 17 Preparation Products And Raw materials
Raw materials
Preparation Products
BTK inhibitor 17 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Hebei Miaoyin Technology Co.,Ltd | +86-17367732028 +86-17367732028 | kathy@hbyinsheng.com | China | 3582 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Jiangsu shring Biopharma Co., Ltd. | +8613372282299 | sales@shringchem.com | China | 3545 | 58 |
| Chuzhou KeMail Chemical Technology Co., Ltd | 0550-5196001 15000891977 | wj520wjxby@126.com | China | 1836 | 55 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7892 | 56 |
| InvivoChem | 13549236410 | sales@invivochem.cn | China | 6713 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24018 | 58 |