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.
JAK3-IN-9
Catalog No. T61814 CAS
1430095-30-9
JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].
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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
JAK3-IN-9 is a potent and orally active inhibitor of the Janus kinase 3 (JAK3) enzyme, displaying an impressive IC50 value of 1.7 nM. It exhibits high selectivity towards the JAK3 signaling pathway, making it a valuable tool for studying autoimmune diseases. Additionally, JAK3-IN-9 possesses desirable characteristics such as low toxicity and excellent oral bioavailability. It also demonstrates promising anti-arthritis activity, thus enhancing its potential as a therapeutic agent [1].
In vitro
JAK3-IN-9 (compound 11i) exhibits a high level of selective inhibition towards JAK3, achieving an IC50 value of 1.7 nM [1]. In Cell Viability Assays using PBMCs at a concentration of 1 μM and an incubation time of 30 minutes, it demonstrated preferential inhibition of JAK3 [1].
In vivo
JAK3-IN-9, referred to as compound 11i, demonstrated selective inhibition of JAK3 cytokine signaling in primary cells when administered orally at dosages of 3, 10, and 30 mg/kg to female Lewis rats once daily for 20 days. Additionally, it exhibited a high area under the curve (AUC) of 2104 μg/ml, increased the half-life to 2.56 hours, and showed favorable oral bioavailability of 48% upon a single intravenous injection at 1 mg/kg in male DBA1j mice aged 8 to 12 weeks. Furthermore, JAK3-IN-9 significantly reduced paw swelling in a dose-dependent manner, with an effective dose (ED50) value of 10 mg/kg, after oral administration once daily for 20 days at a dose of 30 mg/kg. These results, obtained from studies conducted on male DBA1j mice and female Lewis rats, indicate its potential as an anti-arthritis agent in the CIA mice model.
Molecular Weight
393.46
Formula
C17H23N5O4S
CAS No.
1430095-30-9
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.