Apilimod dimesylate

Cat. No. 7283 1 次引用提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent and selective PIKfyve inhibitor

化学名： 4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate

纯度： ≥98% (HPLC)

引用文献 (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 Apilimod dimesylate

Apilimod dimesylate is a potent and selective PIKfyve inhibitor (IC₅₀ = 14 nM). Exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. Apilimod dimesylate reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. Also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells. Inhibits production of IL-12 and IL-23. In motor neurons derived from patients with amyotrophic lateral sclerosis (ALS) Apilimod dimesylate promotes exocytosis of neurotoxic proteins and in mouse ALS models, the compound reduces pathology and prolongs survival. Anti-inflammatory. Water-soluble.

化合物库 for Apilimod dimesylate

Apilimod dimesylate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Apilimod dimesylate

分子量	610.7
公式	C₂₃H₂₆N₆O₂.2CH₃SO₃H
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	870087-36-8
PubChem ID	91885471
InChI Key	GAJWNIKZLYZYSY-OKUPSQOASA-N
Smiles	C[S](O)(=O)=O.C[S](O)(=O)=O.CC1=CC=CC(\C=N\NC2=CC(=NC(OCCC3=CC=CC=N3)=N2)N2CCOCC2)=C1

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 Apilimod dimesylate

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	water	61.07	100
	DMSO	30.53	50

制备储备液 for Apilimod dimesylate

以下数据基于产品分子量 610.7。 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	1.64 mL	8.19 mL	16.37 mL
5 mM	0.33 mL	1.64 mL	3.27 mL
10 mM	0.16 mL	0.82 mL	1.64 mL
50 mM	0.03 mL	0.16 mL	0.33 mL

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产品说明书 for Apilimod dimesylate

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Apilimod dimesylate

参考文献是支持产品生物活性的出版物。

Wada et al (2007) Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood 109 1156 PMID: 17053051

Cai et al (2013) PIKfyve, a class III PI-kinase, is the target of the small molecular IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling. Chem.Biol. 20 912 PMID: 23890009

Riva et al (2020) Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing. Nature 586 113 PMID: 32707573

Ou et al (2020) Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. Nat.Commun. 11 1620 PMID: 32221306

Gayle et al (2017) Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood 129 1768 PMID: 28104689

Hung et al (2023) PIKFYVE inhibition mitigates disease in models of diverse forms of ALS. Cell PMID: 36754049

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

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关键词: Apilimod dimesylate, Apilimod dimesylate supplier, Phosphatidylinositol, 3-phosphate, 5-kinase, PIKfyve, inhibitors, inhibits, potent, selective, SARS-COV-2, COVID-19, B, cell, non-hodgkin, lymphoma, NHL, interleukins, IL-23, IL-12, amyotrophic, lateral, sclerosis, ALS, induces, exocytosis, Other, Kinases, Endocytosis, Cytokines, Coronavirus, Exocytosis, 7283, Tocris Bioscience

1 篇 Apilimod dimesylate 的引用文献

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

Markku et al (2023) SARS-CoV-2 Infection of Human Neurons Is TMPRSS2 Independent, Requires Endosomal Cell Entry, and Can Be Blocked by Inhibitors of Host Phosphoinositol-5 Kinase. J Virol 97 e0014423 PMID: 37039676

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