Peficitinib
- CAS No.
- 944118-01-8
- Chemical Name:
- Peficitinib
- Synonyms
- Carotegrast methyl;1H-Pyrrolo[2,3-b]pyridine-5-carboxamide, 4-[(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)amino]-, stereoisomer;CS-2584;Peficitinib;JNJ-54781532;JNJ-54781533;Peficitinib ASP015K;ASP015K;JNJ-54781532;Piraxostat Impurity 34;Peficitinb (ASP015K, JNJ-54781532)
- CBNumber:
- CB32730346
- Molecular Formula:
- C18H22N4O2
- Molecular Weight:
- 326.39
- MOL File:
- 944118-01-8.mol
- Modify Date:
- 2024/7/2 8:55:06
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P280-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Peficitinib Chemical Properties,Uses,Production
Characteristics
Class: non-receptor tyrosine kinase
Treatment: rheumatoid arthritis
Elimination half-life = 9.4 ± 7.4 h
Protein binding = 73–75%
Uses
Peficitinib can be used in therapeutic use and biological study of codrug and preparation of bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators.
brand name
SmyrafTM
Enzyme inhibitor
This orally bioavailable JAK inhibitor and anti-rheumatoid arthritis drug (FW = 326.39 g/mol; CAS 944118-01-8; Solubility: 200 mM in DMSO), also named ASP015K, JNJ-54781532, and trans-4-[[5-hydroxy-2- adamantyl]amino]-1H-pyrrolo[2,3-b]pyridine-5-carboxamide, targets Janus Kinase JAK1, JAK2, JAK3 and the nonreceptor tyrosine kinase Tyk2 enzyme with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM, respectively. Itsselectively suppress JAK3 or JAK1/2, respectively, may explain the weaker effects on red blood cells and platelets reported to be caused by JAK2 inhibition. Moreover, peficitinib improves symptoms in RA animal models after once-daily oral administration and demonstrates dosedependent improvement in psoriatic disease activities in a 6-week phase IIa study. The terminal mean half-life of peficitinib is 7–13 hours in pharmacological studies with healthy subjects
Metabolism
Peficitinib exhibited low aqueous solubility (≤0.1 mg/mL at pH 7) and modest cell permeability. It also showed moderate oral bioavailability in rats (46%) and monkeys (19%). In healthy volunteers, a single oral dose of 150 mg peficitinib showed an elimination half-life of 9.4 h and high clearance (CL/F = 85.7 L/h, 78% of human hepatic blood flow = 109 L/h for 70 kg body weight). Following oral administration, the major metabolites in humans were the sulfate conjugate 9 and N-methyl conjugate 11 via human sulfotransferase SULT2A1 and nicotinamide N-methyltransferase (NNMT). Peficitinib was cleared through multiple pathways (renal and possibly biliary excretion, and metabolism) with no prevalent single mechanism.
Peficitinib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32760 | 60 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29826 | 58 | Inquiry |
| Fuxin Pharmaceutical | +86-021-021-50872116 +8613122107989 | China | 10297 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
| Alfa Chemistry | +1-5166625404 | United States | 21317 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| RR Scientific LLC | +86-13917743231 | United States | 878 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 | United States | 19973 | 58 | Inquiry |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | China | 11681 | 58 | Inquiry |