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DG051

目录号: PL13315 纯度: ≥99%

DG051 是一种有效的白三烯 A4 水解酶 (leukotriene A4 hydrolase) 抑制剂，IC50 为 47 nM。

CAS No. :929915-58-2

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中文名称	DG051
中文别名	DG 051 (HCl salt)
英文名称	DG051
英文别名	DG 051 (HCl salt);4-{(S)-2-(4-(4-chlorophenoxy)phenoxymethyl)pyrrolidin-1-yl}-1-butyric acid hydrochloride;NULL;DG 051;DG-051;4-((S)-2-((4-(4-chlorophenoxy)phenoxy)Methyl)pyrrolidin-1-yl)butanoic acid hydrochloride;DG051;28B7Y5Y8EF;UCPVOTSNNAVKNE-LMOVPXPDSA-N;SB18806;4-{(S)-2-[4-(4-chloro-phenyoxy)-phenoxymethyl]-pyrrolidin-1-yl}-butyric acid HCl salt;4-{(S)-2-[4-(4-Chloro-phenoxy)-phenoxymethyl]-pyrrolidin-1-yl}-butyric acid hydrochloride;(2S)-2-[[4-(4-Chlorophenoxy)phenoxy]methyl]-1-pyrrolidinebutanoicAci;(S)-4-(2-((4-(4-Chlorophenoxy)phenoxy)methyl)pyrrolidin-1-yl)butanoic acid hydrochloride
Cas No.	929915-58-2
分子式	C₂₁H₂₅Cl₂NO₄
分子量	426.33
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	DG051 是一种有效的白三烯 A4 水解酶 (leukotriene A4 hydrolase) 抑制剂，IC50 为 47 nM。

产品详情	DG051 是一种有效的白三烯 A4 水解酶 (leukotriene A4 hydrolase) 抑制剂，IC₅₀ 为 47 nM。
生物活性	DG051 is a potent leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis in the enzyme assay with an IC 50 =47 nM.
性状	Solid
IC50 & Target[1][2]	IC50: 47 nM (LTA4H)
体外研究(In Vitro)	DG051 is a potent inhibitor of LTA4H aminopeptidase activity against L-alanine p-nitroanilide (IC50=72 nM). DG051 inhibits human whole blood (HWB) with IC50 of 37 nM. As applied within the context of LTA4H inhibitor design, the chemistry team is able to design a potent DG051(Kd=26 nM) with high aqueous solubility (>30 mg/mL) and high oral bioavailability (>80% across species) that is currently undergoing clinical evaluation for the treatment of myocardial infarction and stroke DG-051 is a first-in-class small molecule inhibitor of leukotriene A4 hydrolase (LTA4H), currently in Phase II clinical development for the prevention of heart attack. 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	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Sandanayaka V, et al. Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis. J Med Chem. 2010 Jan 28;53(2):573-85. [2]. Enache LA, et al. Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6275-9.

溶解度数据	In Vitro: DMSO : ≥ 325 mg/mL (762.32 mM)配制储备液

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[1]. Sandanayaka V, et al. Discovery of 4-[(2S)-2-{[4-(4-chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic acid (DG-051) as a novel leukotriene A4 hydrolase inhibitor of leukotriene B4 biosynthesis. J Med Chem. 2010 Jan 28;53(2):573-85.
[2]. Enache LA, et al. Synthesis and structural assignment of two major metabolites of the LTA4H inhibitor DG-051. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6275-9.

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。

DG051

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