TPCA-1

Cat. No. 2559 8 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent, selective inhibitor of IKKβ

化学名： 2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide

纯度： ≥97% (HPLC)

说明书

引用文献 (8)

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 TPCA-1

TPCA-1 is a potent, selective inhibitor of IκB kinase (IKK) β (IC₅₀ = 17.9 nM) that displays > 22-fold selectivity over IKKα and > 550-fold selectivity over other kinases and enzymes. Inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF-κB nuclear localization. Reduces the severity and onset of collagen-induced arthritis; anti-inflammatory.

化合物库 for TPCA-1

TPCA-1 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。

技术数据 for TPCA-1

分子量	279.29
公式	C₁₂H₁₀FN₃O₂S
储存	Store at -20°C
纯度	≥97% (HPLC)
CAS Number	507475-17-4
PubChem ID	9903786
InChI Key	SAYGKHKXGCPTLX-UHFFFAOYSA-N
Smiles	NC(=O)NC1=C(C=C(S1)C1=CC=C(F)C=C1)C(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 TPCA-1

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	27.92	100

制备储备液 for TPCA-1

以下数据基于产品分子量 279.29。 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	3.58 mL	17.9 mL	35.81 mL
5 mM	0.72 mL	3.58 mL	7.16 mL
10 mM	0.36 mL	1.79 mL	3.58 mL
50 mM	0.07 mL	0.36 mL	0.72 mL

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产品说明书 for TPCA-1

分析证书/产品说明书

化学品安全技术说明书

参考文献 for TPCA-1

参考文献是支持产品生物活性的出版物。

Podolin et al (2005) Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IκB kinase 2, TPCA-1 (2-[aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and J.Pharmacol.Exp.Ther. 312 373 PMID: 15316093

Birrell et al (2005) IK-B kinase-2 inhibitor blocks inflammation in human airway smooth muscle and a rat model of asthma. Am.J.Respir.Crit.Care Med. 172 962 PMID: 16002568

Birrell et al (2006) IκB kinase-2-independent and-dependent inflammation in airway disease models: relevance of IKK-2 inhibition to the clinic. Mol.Pharmacol. 69 1791 PMID: 16517756

If you know of a relevant reference for TPCA-1, please let us know.

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