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

Chemical Structure : Tofimilast

CAS No.: 185954-27-2

Tofimilast (CP-325366, CP325366)

货号: PC-63090Not For Human Use, Lab Use Only.

Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively.

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

生物&药学活性

Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively.
Tofimilast (CP-325366) shows weakly or no inhibition for PDE4C, and no activity for PDE1, PDE2, PDE3, PDE5, PDE6, and PDE7.
Tofimilast (CP-325366) increases cAMP levels in PGE1-stimulated U937 cells with an EC50 of 230 nM, inhibits human monocyte PDE mediated cAMP catabolism with an IC50 of 67 nM and LPS stimulated human monocyte TNFα release with an IC50 of 59 nM.
Tofimilast (CP-325366) shows low oral bioavailability and no emesis-associated behaviors in the ferret emesis model.

物理化学性质&存储条件

分子量 339.461
分子式 C18H21N5S
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

9-Cyclopentyl-7-ethyl-3-(thiophen-2-yl)-6,9-dihydro-5H-pyrazolo(3,4-c)-1,2,4-triazolo(4,3-a)pyridine

参考文献

1. Duplantier AJ, et al. J Med Chem. 2007 Jan 25;50(2):344-9.

2. Giembycz MA. Br J Pharmacol. 2008 Oct;155(3):288-90.

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