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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-CHF6001
CHF6001

Chemical Structure : CHF6001

CAS No.: 1239278-59-1

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CHF6001 (Tanimilast, CHF-6001)

货号: PC-60725Not For Human Use, Lab Use Only.

Tanimilast (CHF6001) is a novel, highly potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 0.026 nM.

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2 mg ￥1980 In stock
5 mg ￥3280 In stock
10 mg ￥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tanimilast (CHF6001) is a novel, highly potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 0.026 nM.
CHF6001 inhibits PDE4 isoforms A-D with equal potency, 7- and 923-fold more potent than roflumilast and cilomilast, and displays >20,000-fold selectivity versus PDE4 compared with a panel of PDEs.
CHF6001 effectively inhibits (subnanomolar IC50 values) the release of TNF-α from human PBMCs, THP-1, and rodent macrophages.
CHF6001 inhibitsLPS-induced pulmonary neutrophilia (ED50=0.205 uM/kg) and leukocyte infiltration (ED50=0.188 uM/kg) in rats.

物理化学性质&存储条件

分子量 687.533
分子式 C30H30Cl2F2N2O8S
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

(S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyloxy)ethyl)pyridine 1-oxide

参考文献

1. Armani E, et al. J Med Chem. 2014 Feb 13;57(3):793-816.

2. Villetti G, et al .J Pharmacol Exp Ther. 2015 Mar;352(3):568-78.

3. Moretto N, et al. J Pharmacol Exp Ther. 2015 Mar;352(3):559-67.

4. Edwards MR, et al. Pharmacol Res Perspect. 2016 Jan 15;4(1):e00202.

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