This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Peficitinib hydrochloride
Catalog No. T61365 CAS
1353219-06-3
Peficitinib hydrochloride, also known as ASP015K, is an orally active JAK inhibitor compound. It exhibits inhibitory activity against JAK1, JAK2, JAK3, and Tyk2, with IC 50 values of 3.9, 5.0, 0.7, and 4.8 nM, respectively.
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
Peficitinib hydrochloride, also known as ASP015K, is an orally active JAK inhibitor compound. It exhibits inhibitory activity against JAK1, JAK2, JAK3, and Tyk2, with IC 50 values of 3.9, 5.0, 0.7, and 4.8 nM, respectively.
In vitro
Peficitinib hydrobromide, administered at concentrations ranging from 0 to 100 nM for three days, effectively suppresses IL-2-induced T cell proliferation in a concentration-dependent fashion, with an IC 50 of 10 nM, as demonstrated in a Cell Proliferation Assay using splenocytes from male Lewis rats [1]. Additionally, at concentrations between 10 to 1000 nM, it impedes IL-2-induced STAT5 phosphorylation, displaying a mean IC 50 of 124 nM in rat whole blood and 127 nM in human lymphocytes, indicating its inhibitory action on STAT5 phosphorylation in both rat and human cells [1].
In vivo
Peficitinib hydrobromide administered orally at doses ranging from 1-30 mg/kg once daily for 24 days demonstrated dose-dependent efficacy in both prophylactic and therapeutic protocols within an adjuvant-induced arthritis (AIA) rat model. Using seven-week-old female Lewis rats, the study quantitatively assessed the compound’s impact on disease markers: it significantly reduced paw volume starting at 1 mg/kg, with an ED50 of 2.7 mg/kg (95% confidence interval: 1.5–4.2 mg/kg), and notably decreased bone destruction scores at doses of 10 mg/kg or higher. At the maximum dose of 30 mg/kg, peficitinib hydrobromide effectively mitigated both paw swelling and bone damage, showcasing substantial therapeutic potential in the AIA model.
Molecular Weight
362.86
Formula
C18H23ClN4O2
CAS No.
1353219-06-3
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
Tween 80,mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL Corn oil,mix and clarify.
Note:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.