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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-CI-1044
CI-1044

Chemical Structure : CI-1044

CAS No.: 197894-84-1

CI-1044 (CI1044)

货号: PC-62897Not For Human Use, Lab Use Only.

CI-1044 is a potent, selective and orally bioavailable PDE4 inhibitor with IC50 of 0.27 uM, displays high selectivity for PDE4 versus PDE1/3/5, and no PDE4 subtype (4A-D) selectivities.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CI-1044 is a potent, selective and orally bioavailable PDE4 inhibitor with IC50 of 0.27 uM, displays high selectivity for PDE4 versus PDE1/3/5, and no PDE4 subtype (4A-D) selectivities.
CI-1044 exhibits efficient in vitro inhibition of TNFα release from hPBMC and hWB with IC50 of 0.34 and 0.84 uM, respectively.
CI-1044 exhibits potent in vivo activity in antigen-induced eosinophil recruitment in rats (ED50=3.2 mg/kg, p.o.).

物理化学性质&存储条件

分子量 397.438
分子式 C23H19N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-N-(9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-3-yl)nicotinamide

参考文献

1. Burnouf C, et al. J Med Chem. 2000 Dec 14;43(25):4850-67.

2. Ouagued M, et al. Pulm Pharmacol Ther. 2005;18(1):49-54.

3. Hanton G, et al. Toxicol Lett. 2008 Jun 10;179(1):15-22.

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