Atuliflapon|2041075-86-7|(AZD5718)-陌孚医药/Medlife

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Atuliflapon (Synonyms: AZD5718)

目录号: PL02578 纯度: ≥98%

CAS No. :2041075-86-7

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中文名称	Atuliflapon
英文名称	Atuliflapon
英文别名	AZD5718;(1R,2R)-2-(4-(5-Methyl-1H-pyrazol-3-yl)benzoyl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-3-yl)cyclohexane-1-carboxamide;GTPL10352;US10183947, Example 7;BDBM323023;BDBM50524102;compound 12 [PMID: 30869888];(1R,2R)-2-[4-(3-Methyl-1H-pyrazol-5- yl)benzoyl]-N-(4-oxo-4,5,6,7- tetrahydropyrazolo[1,5-a]pyrazin-3- yl)cyclohexanecarboxamide;(1R,2R)-2-[4-(5-methyl-1H-pyrazol-3-yl)benzoyl]-N-(4-oxo-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-3-yl)cycloh;Chembl4542281;Atuliflapon
Cas No.	2041075-86-7
分子式	C₂₄H₂₆N₆O₃
分子量	446.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Atuliflapon (AZD5718) 是具有口服活性的 FLAP (5 -脂氧合酶激活蛋白) 的抑制剂，其 IC₅₀ 值为 2 nM。Atuliflapon 可用于冠状动脉疾病的研究。

生物活性

Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5?Lipoxygenase activating protein), with an IC 50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.

性状

Solid

IC50 & Target[1][2]

IC50: 2 nM (FLAP).

体外研究(In Vitro)

Atuliflapon demonstrates a dose dependent and greater than 90% suppression of leukotriene production over 24 h.
Atuliflapon exhibits an IC50 of 39 nM for LTB4. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Atuliflapon exhibits t1/2 of 0.45 h and 2.1 h in rat and dog by iv injection, respectively.
Atuliflapon shows no inhibition of 5-LO pathway activity in rodent blood. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Daniel Pettersen, et al. Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease. J Med Chem. 2019 May 9;62(9):4312-4324.

溶解度数据	In Vitro: DMSO : 125 mg/mL (279.96 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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