TAK 242

Cat. No. 6587 6 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： TLR4 signaling inhibitor

化学名： (R)-Ethyl 6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate

纯度： ≥98% (HPLC)

引用文献 (6)

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 TAK 242

TAK 242 is a toll-like receptor 4 (TLR4) signaling inhibitor. Binds to intracellular domain of TLR4. Inhibits LPS-induced cytokine production in vitro (IC₅₀ values are 1.3, 1.3 and 3.2 nM for IL-6, TNFα and NO production). Reduces lesion volume in a mouse model of cerebral cavernous malformations (CCMs). Also attenuates increased cytokine levels in a mouse sepsis model, when given in combination with ceftazidime. Cell permeable.

技术数据 for TAK 242

分子量	361.82
公式	C₁₅H₁₇ClFNO₄S
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	243984-11-4
PubChem ID	11703255
InChI Key	LEEIJTHMHDMWLJ-CQSZACIVSA-N
Smiles	CCOC(C1=CCCC[C@H]1S(=O)(NC2=C(C=C(C=C2)F)Cl)=O)=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 TAK 242

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	36.18	100
	ethanol	36.18	100

制备储备液 for TAK 242

以下数据基于产品分子量 361.82。 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	2.76 mL	13.82 mL	27.64 mL
5 mM	0.55 mL	2.76 mL	5.53 mL
10 mM	0.28 mL	1.38 mL	2.76 mL
50 mM	0.06 mL	0.28 mL	0.55 mL

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产品说明书 for TAK 242

分析证书/产品说明书

化学品安全技术说明书

参考文献 for TAK 242

参考文献是支持产品生物活性的出版物。

Yamada et al (2005) Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate. J.Med.Chem. 48 7457 PMID: 16279805

Ii et al (2006) A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signal Mol.Pharmacol. 69 1288 PMID: 16373689

Tang et al (2017) Endothelial TLR4 and the microbiome drive cerebral cavernous malformations. Nature 545 305 PMID: 28489816

Takashima et al (2009) Analysis of binding site for the novel small-molecule TLR4 signal transduction inhibitor TAK-242 and its therapeutic effect on mouse sepsis model. Br.J.Pharmacol. 157 1250 PMID: 19563534

If you know of a relevant reference for TAK 242, please let us know.

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关键词: TAK 242, TAK 242 supplier, TAK242, toll, like, receptor, TLR4, signaling, inhibitor, inhibits, sepsis, cell, permeable, Toll-like, Receptors, 6587, Tocris Bioscience

6 篇 TAK 242 的引用文献

引用文献是使用了 Tocris 产品的出版物。 TAK 242 的部分引用包括：

Grigoryeva et al (2021) Human macrophages utilize a wide range of pathogen recognition receptors to recognize Legionella pneumophila, including Toll-Like Receptor 4 engaging Legionella lipopolysaccharide and the Toll-like Receptor 3 nucleic-acid sensor PLoS 17 e1009781 PMID: 34280250

Avadhesha et al (2023) TLR4 activation by lysozyme induces pain without inflammation. Front Immunol 14 1065226 PMID: 37197666

Titus Ikusya et al (2022) Bodyweight, locomotion, and behavioral responses of the naked mole rat (Heterocephalus glaber) to lipopolysaccharide administration. J Comp Physiol A Neuroethol Sens Neural Behav Phys 208 493-504 PMID: 35731263

Harpal S et al (2022) Asprosin Exerts Pro-Inflammatory Effects in THP-1 Macrophages Mediated via the Toll-like Receptor 4 (TLR4) Pathway. Int J Mol Sci 24 PMID: 36613673

Emre et al (2022) Opioid Antagonist Nanodrugs Successfully Attenuate the Severity of Ischemic Stroke. Mol Pharm 19 2254-2267 PMID: 35506882

Robert A et al (2022) Human platelets display dysregulated sepsis-associated autophagy, induced by altered LC3 protein-protein interaction of the Vici-protein EPG5. Autophagy 18 1534-1550 PMID: 34689707

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Pathways for TAK 242

Toll-like Receptor Signaling Pathway

TLR signaling is involved in the cellular response to threatening molecules such as bacteria and viruses. It results in an inflammatory and immmunological response.