Peficitinib hydrobromide
- Product Name
- Peficitinib hydrobromide
- CAS No.
- 1353219-05-2
- Chemical Name
- Peficitinib hydrobromide
- Synonyms
- RMA-849;Peficitinib Hydrobromid;Peficitinib hydrobromide;Peficitinib hydrobromide (JAN/USAN);anti-4-((5-Hydroxyadamantan-2-yl)amino)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide hydrobromide;4-(5-Hydroxytricyclo3.3.1.13,7dec-2-yl)amino-1H-pyrrolo2,3-bpyridine-5-carboxamide hydrobromide (1:1) stereoisomer
- CBNumber
- CB14848254
- Molecular Formula
- C18H22N4O2. HBr
- Formula Weight
- 407.31
- MOL File
- 1353219-05-2.mol
Peficitinib hydrobromide Property
- InChI
- InChI=1S/C18H22N4O2.BrH/c19-16(23)13-8-21-17-12(1-2-20-17)15(13)22-14-10-3-9-4-11(14)7-18(24,5-9)6-10;/h1-2,8-11,14,24H,3-7H2,(H2,19,23)(H2,20,21,22);1H
- InChIKey
- ZUVPMAPXNYGJQC-UHFFFAOYSA-N
- SMILES
- N(C1C(=CN=C2NC=CC=12)C(=O)N)C1C2CC3CC(O)(C2)CC1C3.Br
Peficitinib hydrobromide Chemical Properties,Usage,Production
Uses
Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively[1].
Mechanism of action
Peficitinib hydrobromide potently inhibits the JAK-STAT pathway and blocks the signaling of pro-inflammatory cytokines such as IL-6 and IFN-γ. It has the strongest inhibitory activity against JAK3 (IC₅₀ = 0.7 nM), while also taking into account other subtypes (JAK1/2/Tyk2 IC₅₀ 3.9–5.0 nM).
Synthesis
Synthesis of Peficitinib hydrobromide
in vivo
Peficitinib hydrobromide (1-30 mg/kg; p.o.; once daily for 24 days) shows dose-dependent efficacy both in prophylactic and therapeutic dosing regimens in an adjuvant-induced arthritis rat model[1].
| Animal Model: | Seven-weeks-old female Lewis rats, adjuvant-induced arthritis (AIA) model[1] |
| Dosage: | 1, 3, 10, and 30 mg/kg |
| Administration: | Oral administration, once daily for 24 days |
| Result: | Significantly inhibited the increase in paw volume at doses of 1 mg/kg or greater with an ED50 value of 2.7 mg/kg (95% confidence interval: 1.5–4.2 mg/kg). Significantly reduced the bone destruction score at 10 mg/kg or greater and almost fully ameliorated both paw swelling and bone destruction scores at 30 mg/kg. |
IC 50
JAK3: 0.7 nM (IC50); JAK1: 3.9 nM (IC50); Tyk2: 4.8 nM (IC50); JAK2: 5 nM (IC50)
References
[1] Ito M, et al. A novel JAK inhibitor, peficitinib, demonstrates potent efficacy in a rat adjuvant-induced arthritis model. J Pharmacol Sci. 2017 Jan;133(1):25-33. DOI:10.1016/j.jphs.2016.12.001
Peficitinib hydrobromide Preparation Products And Raw materials
Raw materials
Preparation Products
Peficitinib hydrobromide Suppliers
View Lastest Price from Peficitinib hydrobromide manufacturers
- Product
- Peficitinib hydrobromide 1353219-05-2
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 98%
- Supply Ability
- 1000kg
- Release date
- 2025-11-12
- Product
- Peficitinib Hydrobromide 1353219-05-2
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2025-09-10
- Product
- Peficitinib hydrobromide 1353219-05-2
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 98%
- Supply Ability
- 1000kg
- Release date
- 2025-06-12