CE-224535|724424-43-5|-陌孚医药/Medlife

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CE-224535

目录号: PL08680 纯度: ≥98%

CAS No. :724424-43-5

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中文名称	CE-224535
英文名称	CE-224535
英文别名	Benzamide,2-chloro-5-[4,5-dihydro-4-[(2R)-2-hydroxy-3-methoxypropyl]-3,5-dioxo-1,2,4-triazin-2(3H)-yl]-N-[(1-hydroxycycloheptyl)methyl]-;2-chloro-N-[(1-hydroxycycloheptyl)methyl]-5-[4-[(2R)-2-hydroxy-3-methoxypropyl]-3,5-dioxo-1,2,4-triazin-2-yl]benzamide;Benzamide,2-chloro-5-[4,5-dihydro-4-[(2R)-2-hydroxy-3-methoxypropyl]-3,5-dioxo-1,2,4-triazin-2(3H)-yl]-N-[(1-hydroxycyclohept;2-(4-Chloro-3-(3-(1-hydroxycycloheptyl)propanoyl)phenyl)-4-((2R)-2-hydroxy-3-methoxy-propyl)-1,2,4-triazine-3,5-dione;Benzamide, 2-chloro-5-(4,5-dihydro-4-((2R)-2-hydroxy-3-methoxypropyl)-3,5-dioxo-1,2,4-triazin-2(3H)-yl)-n-((1-hydroxycycloheptyl)methyl)-;CE 224,535;CE-224535;CHEMBL1823817;SureCN3475321;UNII-T8B02RAU3C
Cas No.	724424-43-5
分子式	C₂₂H₂₉N₄O₆Cl
分子量	480.94
包装储存	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

CE-224535 是一个有选择性的 P2X₇ 受体拮抗剂。

生物活性

CE-224535 is a selective P2X 7 receptor antagonist.

性状

Solid

IC50 & Target[1][2]

P2X7 receptor

体外研究(In Vitro)

CE-224535 is developed as a disease-modifying antirheumatic drugs (DMARD) and is a selective antagonist of the human P2X7 receptor. CE-224535 can reduce leukocyte secretion of IL-1 and IL-18, thereby providing a novel therapeutic approach for treatment of rheumatoid arthritis (RA). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In rats, CE-224535 has low CL p (11 mL/min/kg) and a large V dss of 7.6 L/kg, which results in a half-life of 2.4 h. Upon oral administration to rats at 5 mg/kg, CE-224535 provides maximal plasma exposure (C max ) that is ~90 fold over its IC 90 in human blood (C max =0.21 μg/mL or 0.44 μM). The oral bioavailability of CE-224535 is low in rats (F=2.6%), but this is believed to be a rat specific phenomenon since corresponding oral bioavailability in both dog (59%) and monkey (22%) is adequate. 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

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Stock TC, et al. Efficacy and safety of CE-224,535, an antagonist of P2X7 receptor, in treatment of patients with rheumatoid arthritis inadequately controlled by methotrexate. J Rheumatol. 2012 Apr;39(4):720-7.
[2]. Duplantier AJ, et al. Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3708-11

溶解度数据	In Vitro: DMSO : 100 mg/mL (207.93 mM; Need ultrasonic)配制储备液

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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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