BAY-X 1005|128253-31-6|(BAY X 1005; DG-031)-陌孚医药/Medlife

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BAY-X 1005 (Synonyms: BAY X 1005; DG-031)

目录号: PC11564 纯度: ≥98%

CAS No. :128253-31-6

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中文名称

BAY-X 1005

英文名称

BAY-X 1005

英文别名

Benzeneacetic acid, a-cyclopentyl-4-(2-quinolinylmethoxy)-,(aR)-;(2R)-2-cyclopentyl-2-[4-(quinolin-2-ylmethoxy)phenyl]acetic acid;BAY X1005;BAY-X 1005;BAY-X-1005;Bayx-1005;DG-031;Veliflapon;α-Cyclopentyl-4-(2-quinolinylmethoxy)-(R)-benzeneacetic acid;(αR)-α-Cyclopentyl-4-(2-quinolinylmethoxy)-benzeneacetic acid;DG 031;Velifapon;BAY 1005;ZEYYDOLCHFETHQ-JOCHJYFZSA-N;2-(4-(quinolin-2-yl-methoxy)phenyl)-2-cyclopentylacetic acid

Cas No.

128253-31-6

分子式

C₂₃H₂₃NO₃

分子量

361.43

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

性状

Solid

IC50 & Target[1][2]

LTB₄

LTC₄

体外研究(In Vitro)

Veliflapon (BAY X 1005; DG-031) effectively inhibits the synthesis of LTB4 in A23187-stimulated leukocytes from rats, mice and humans (IC₅₀s of 0.026, 0.039 and 0.22 μM, respectively) as well as the formation of LTC4 (IC₅₀ of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis.
Veliflapon after topical (18 μg/ear) and oral (48.7 mg/kg) administration has antiedematous effects in the arachidonic acid-induced mouse ear inflammation test.
Veliflapon is potent (11.8 and 6.7 mg/kg p.o. at 1 and 5 hours, respectively) and has a long duration of action (ED₄₀ of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female apoE/LDLR-DKO mouse model
Dosage:	18.8 mg/kg
Administration:	Diet; per day during 16 weeks
Result:	Inhibited atherogenesis.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Hatzelmann A, et al. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X 1005: implications for biological regulation of 5-lipoxygenase. Agents Actions. 1994 Nov;43(1-2):64-8. [Information]

[2]. Müller-Peddinghaus R, et al. BAY X1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. J Pharmacol Exp Ther. 1993 Oct;267(1):51-7. [Information]

[3]. Fruchtmann R, et al. 体外研究 pharmacology of BAY X1005, a new inhibitor of leukotriene synthesis. Agents Actions. 1993 Mar;38(3-4):188-95. [Information]

[4]. Jawień J, et al. BAY x 1005 attenuates atherosclerosis in apoE/LDLR - double knockout mice. J Physiol Pharmacol. 2007 Sep;58(3):583-8. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (276.68 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7668 mL	13.8339 mL	27.6679 mL
5 mM	0.5534 mL	2.7668 mL	5.5336 mL
10 mM	0.2767 mL	1.3834 mL	2.7668 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

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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