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Darapladib Sale

(Synonyms: N-[2-(二乙氨基)乙基]-N-[4'-(三氟甲基)-1,1'-联苯-4-甲基]-2-[2-(4-氟苄硫基)-4-氧代-4,5,6,7-四氢-1H-环戊并[D]嘧啶-1-基]乙酰胺,SB-480848;SB480848;SB 480848) 目录号 : GC12361

A reversible inhibitor of Lp-PLA2

Darapladib Chemical Structure

Cas No.:356057-34-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,271.00
现货
5mg
¥767.00
现货
25mg
¥3,119.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Animal experiment:

Mice[2] Male homozygous LDLR-deficient mice (C57/Bl6 genetic background) are fed a high-fat diet consisting of 18% hydrogenated cocoa butter, 0.15% cholesterol, 7% casein, 7% sucrose, and 3% maltodextrin for 17 weeks, beginning at 6 weeks of age. Forty mice are divided into two groups (n=20 per group) randomly. One group receive Darapladib by gavage (50 mg/kg per day) once daily, while the other group receive the vehicle (saline). During the 6 weeks of treatment, all mice are housed in a room with a 12-h light/dark cycle and are allowed free access to a high-fat diet and water.

References:

[1]. Blackie JA, et al. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70.
[2]. Hu MM, et al. The inhibition of lipoprotein-associated phospholipase A2 exerts beneficial effects against atherosclerosis inLDLR-deficient mice. Acta Pharmacol Sin. 2011 Oct;32(10):1253-1258.

产品描述

Plaque rupture is responsible for the clinical events of ischemic death, myocardial infarction, acute coronary syndromes and ischemic strokes. Lipoprotein-associated phospholipase A2 (Lp-PLA2) seems to play a major role in the development of such high-risk lesions, in both the coronary and carotid arteries. Darapladib is a selective inhibitor of Lp-PLA2.

In vitro: Darapladib potently inhibited Lp-PLA2 with an IC50 of 270 pM. A lack of selectivity against other secretory PLA2s postulated to play a role in atherogenesis had been demonstrated. The percentage inhibition achieved when 1 μM darapladib was evaluated against human secretory PLA2s IIA, V and X, was 0, 0 and 8.7%, respectively [1].

In vivo: Inhibition of lp-PLA2 by darapladib led to attenuation of inflammation in vivo and decreased plaque formation in ApoE-deficient mice, suggesting an anti-atherogenic role during the progression of atherosclerosis [2].

Clinical trial: Darapladib produced sustained inhibition of plasma Lp-PLA2 activity in patients receiving intensive atorvastatin therapy. IL-6 and hs-CRP changes after 12 weeks of darapladib 160 mg suggested a possible reduction in inflammatory burden [3].

References:
[1] Bui QT, Wilensky RL.  Darapladib. Expert Opin Investig Drugs. 2010;19(1):161-8.
[2] Wang WY, Zhang J, Wu WY, Li J, Ma YL, Chen WH, Yan H, Wang K, Xu WW, Shen JH, Wang YP.  Inhibition of lipoprotein-associated phospholipase A2 ameliorates inflammation and decreases atherosclerotic plaque formation in ApoE-deficient mice. PLoS One. 2011;6(8):e23425.
[3] Mohler ER 3rd, Ballantyne CM, Davidson MH, Hanefeld M, Ruilope LM, Johnson JL, Zalewski A; Darapladib Investigators.  The effect of darapladib on plasma lipoprotein-associated phospholipase A2 activity and cardiovascular biomarkers in patients with stable coronary heart disease or coronary heart disease risk equivalent: the results of a multicenter, randomized, double-blind, placebo-controlled study. J Am Coll Cardiol. 2008;51(17):1632-41.

Chemical Properties

Cas No. 356057-34-6 SDF
别名 N-[2-(二乙氨基)乙基]-N-[4'-(三氟甲基)-1,1'-联苯-4-甲基]-2-[2-(4-氟苄硫基)-4-氧代-4,5,6,7-四氢-1H-环戊并[D]嘧啶-1-基]乙酰胺,SB-480848;SB480848;SB 480848
化学名 N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide
Canonical SMILES CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
分子式 C36H38F4N4O2S 分子量 666.77
溶解度 ≥ 32.95 mg/mL in DMSO, ≥ 891 mg/mL in EtOH 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.4998 mL 7.4988 mL 14.9977 mL
5 mM 0.3 mL 1.4998 mL 2.9995 mL
10 mM 0.15 mL 0.7499 mL 1.4998 mL
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