Veliflapon

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Veliflapon

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

128253-31-6

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议

产品名称

BAY X 1005
DG-031

产品介绍

Veliflapon (BAY X 1005; DG-031) 是一种具有口服活性的，选择性的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂。Veliflapon 也是白三烯 B4和C4合成的抑制剂。

生物活性

Veliflapon (BAY X 1005; DG-031) is an orally active and selective5-lipoxygenase activating protein (FLAP)inhibitor^[1]. Veliflapon inhibits the synthesis of theleukotrienes B4andC4^[2].

IC₅₀& Target

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 (IC₅₀of 0.021 μM) in mouse peritoneal macrophages stimulated with opsonized zymosan^[3].

体内研究
(In Vivo)

Veliflapon (BAY X 1005; DG-031; diet; 18.8 mg/kg/day for 16 weeks ) inhibits atherogenesis^[4].
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^[4].
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 (ED₄₀of 16 hours, 70 mg/kg p.o.) in the rat whole blood ex vivo leukotriene B4 inhibition assay^[4].

Animal Model:	Female apoE/LDLR-DKO mouse model^[4]
Dosage:	18.8 mg/kg
Administration:	Diet; per day during 16 weeks
Result:	Inhibited atherogenesis.

Clinical Trial

分子量

361.43

性状

Solid

Formula

C₂₃H₂₃NO₃

CAS 号

128253-31-6

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。