Baricitinib

Cat. No. 7222 提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Pricing	Availability		Qty

说明： Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2

别名： INCB 28050

化学名： 1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile

纯度： ≥98% (HPLC)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for Baricitinib

Baricitinib is a highly potent JAK1 and JAK2 inhibitor (IC₅₀ values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC₅₀ = 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC₅₀ = 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1 in vitro (K_d values are 17.2, 39.8, 134.4 and 68.5 nM, respectively). Inhibits IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T-cells. Displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. In silico modelling predicts inhibition of SARS-CoV-2 cell entry.

化合物库 for Baricitinib

Baricitinib is also offered as part of the Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Baricitinib

分子量	371.42
公式	C₁₆H₁₇N₇O₂S
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	1187594-09-7
PubChem ID	44205240
InChI Key	XUZMWHLSFXCVMG-UHFFFAOYSA-N
Smiles	CCS(=O)(N1CC(C1)(N2C=C(C3=C4C=CNC4=NC=N3)C=N2)CC#N)=O

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.

溶解性数据 for Baricitinib

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	37.14	100

制备储备液 for Baricitinib

以下数据基于产品分子量 371.42。 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	2.69 mL	13.46 mL	26.92 mL
5 mM	0.54 mL	2.69 mL	5.38 mL
10 mM	0.27 mL	1.35 mL	2.69 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

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产品说明书 for Baricitinib

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Baricitinib

参考文献是支持产品生物活性的出版物。

Fridman et al (2010) Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J.Immunol. 184 5298 PMID: 20363976

Sorrell et al (2016) Family-wide structural analysis of human numb-associated protein kinases. Structure. 24 401 PMID: 26853940

Richardson et al (2020) Baricitinib as potential treatment for 2019-nCoV acute respiratory disease. Lancet. 395 e30 PMID: 32032529

If you know of a relevant reference for Baricitinib, please let us know.

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Pathways for Baricitinib

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.