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Submit ReviewUpadacitinib is a potent and selective JAK1 inhibitor (IC50 = 47 nM). In a cellular assay, Upadacitinib shows selectivity for JAK1 over JAK2, JAK3 and TYK2 (IC50 values are 0.014 μM, 0.593 μM, 1860 μM and 2715 μM). In vivo, Upadacitinib suppresses paw swelling and bone destruction in a rat model of arthritis.
分子量 | 380.37 |
公式 | C17H19F3N6O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1310726-60-3 |
PubChem ID | 58557659 |
InChI Key | WYQFJHHDOKWSHR-MNOVXSKESA-N |
Smiles | C(C)[C@H]1[C@@](C=2N3C4=C(N=CC3=NC2)NC=C4)(CN(C(NCC(F)(F)F)=O)C1)[H] |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.04 | 100 | |
ethanol | 19.02 | 50 |
以下数据基于产品分子量 380.37。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.63 mL | 13.15 mL | 26.29 mL |
5 mM | 0.53 mL | 2.63 mL | 5.26 mL |
10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Parmentier et al (2018) In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2 23 PMID: 30886973
If you know of a relevant reference for Upadacitinib, please let us know.
关键词: Upadacitinib, Upadacitinib supplier, Potent, selective, JAK1, JAK2, JAK3, inhibitors, inhibits, janus, kinase, arthritis, in, vivo, JAK, 7783, Tocris Bioscience
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