Upadacitinib

製品コードS8162 バッチS816201

化学情報

	Synonyms	ABT-494	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₇H₁₉F₃N₆O
	分子量	380.37	CAS No.	1310726-60-3
Solubility (25°C)*	体外	DMSO	76 mg/mL (199.8 mM)
		Ethanol	76 mg/mL (199.8 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Upadacitinib is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.
in vitro	Upadacitinib is most potent on JAK1compared to other family members (JAK1 > JAK2 > JAK3 > TYK2). Upadacitinib demonstrates selectivity across a broad panel of 70+ kinases, with only Rock1 and Rock2 demonstrating IC50 values below 1 μM. Consistent with the Ba/F3 cellular data, upadacitinib potently inhibits the JAK1 dependent cytokines IL-6, OSM, IL-2, and IFNγ, as measured by inhibition of STAT phosphorylation^[1].
in vivo	Upadacitinib inhibits disease pathology in rat adjuvant induced arthritis^[1]. It is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine^[2].

製品説明

Upadacitinib is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.

in vitro

Upadacitinib is most potent on JAK1compared to other family members (JAK1 > JAK2 > JAK3 > TYK2). Upadacitinib demonstrates selectivity across a broad panel of 70+ kinases, with only Rock1 and Rock2 demonstrating IC50 values below 1 μM. Consistent with the Ba/F3 cellular data, upadacitinib potently inhibits the JAK1 dependent cytokines IL-6, OSM, IL-2, and IFNγ, as measured by inhibition of STAT phosphorylation^[1].

in vivo

Upadacitinib inhibits disease pathology in rat adjuvant induced arthritis^[1].

It is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NK cells
	濃度	JAK1 (0.045 μM) and JAK2 (0.109 μM)
	反応時間
	実験の流れ
動物実験	動物モデル	Female Lewis rats
	投薬量	10 mg/kg
	投与方法	o.g.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Type 1 interferons and Foxo1 down-regulation play a key role in age-related T-cell exhaustion in mice [ Nat Commun, 2024, 15(1):1718]	PubMed: 38409097
Macrophage re-programming by JAK inhibitors relies on MAFB [ Cell Mol Life Sci, 2024, 81(1):152]	PubMed: 38528207
IL-6 prevents Th2 cell polarization by promoting SOCS3-dependent suppression of IL-2 signaling [ Cell Mol Immunol, 2023, 10.1038/s41423-023-01012-1]	PubMed: 37046042
Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44]	PubMed: 37726797
Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44]	PubMed: 37726797
Stress signalling and STAT1 activation characterize the keratinocytic gene expression pattern in Hidradenitis suppurativa [ J Eur Acad Dermatol Venereol, 2022, 36(12:2488-2498)]	PubMed: 35881108
An epidermal keratinocyte homogenate induced type 2 and proinflammatory cytokine expression in cultured dermal cells [ J Dermatol Sci, 2022, S0923-1811(22)00092-5]	PubMed: 35437207
Impact of Different JAK Inhibitors and Methotrexate on Lymphocyte Proliferation and DNA Damage [ J Clin Med, 2021, 10(7)1431]	PubMed: 33916057
Janus kinase inhibitors ruxolitinib and baricitinib impair glycoprotein-VI mediated platelet function [ Platelets, 2021, 1-12]	PubMed: 34097573
Emerging systemic JAK inhibitors in the treatment of atopic dermatitis: a review of abrocitinib, baricitinib, and upadacitinib [ Drugs Context, 2020, 92020-8-5]	PubMed: 33240390

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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