|4-(((1S,4S)-5-(4-(4-(恶唑-2-基)苯氧基)苄基)-2,5-二氮杂双环[2.2.1]庚-2-基)甲基)苯甲酸|CsnPharm

CAS No.: 943764-99-6

Acebilustat/阿西鲁司特 Catalog No. CSN18849

Synonyms: CTX-4430;ZK-322;EP-501

Acebilustat is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug.

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技术信息

生物活性

描述Leukotriene B4 (LTB4) is a potent chemoattractant of neutrophil migration and activation. Leukotriene A4 hydrolase (LTA4H) is the rate‐limiting enzyme for LTB4 synthesis. Reducing the production of LTB4 via inhibiting LTA4H may be a potential therapeutic approach for anti-inflammatory treatment. Acebilustat is a potent inhibitor of LTA4H. The IC50 value of acebilustat for the inhibition of LTB4 production in human whole blood is 31ng/mL (~0.064μM)^[3]. Acebilustat at a concentration of 0.1μM decreased the count of apical polymorphonuclear neutrophils at 2-, 10- and 18-hour post-transmigration without affecting primary granule exocytosis in these cells^[4].
参考文献

[1] Elborn JS, Horsley A, et al. Phase I Studies of Acebilustat: Biomarker Response and Safety in Patients with Cystic Fibrosis. Clin Transl Sci. 2017 Jan;10(1):28-34.
[2] Elborn JS, Bhatt L, et al. Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction. Clin Transl Sci. 2017 Jan;10(1):20-27.
[3] Elborn JS, Bhatt L, Grosswald R, Ahuja S, Springman EB. Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction. Clin Transl Sci. 2017 Jan;10(1):20-27.
[4] Forrest OA, Ingersoll SA, Preininger MK, Laval J, Limoli DH, Brown MR, Lee FE, Bedi B, Sadikot RT, Goldberg JB, Tangpricha V, Gaggar A, Tirouvanziam R. Frontline Science: Pathological conditioning of human neutrophils recruited to the airway milieu in cystic fibrosis. J Leukoc Biol. 2018 Oct;104(4):665-675.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0767 mL
- 10.3833 mL
- 20.7666 mL
- 5 mM
- 0.4153 mL
- 2.0767 mL
- 4.1533 mL
- 10 mM
- 0.2077 mL
- 1.0383 mL
- 2.0767 mL

技术信息

CAS号

943764-99-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H27N3O4

运输

蓝冰

分子量

481.54

别名

CTX-4430;ZK-322;EP-501;阿西鲁司特

溶解度

DMSO	16.0 mg/mL (33.2 mM) warming

动物实验配方

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