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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-BPN14770
BPN14770

Chemical Structure : BPN14770

CAS No.: 1606974-33-7

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BPN14770 (Zatolmilast, BPN-14770)

货号: PC-35904Not For Human Use, Lab Use Only.

Zatolmilast (BPN14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively.

规格 价格 库存 数量
5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3680 In stock
50 mg ￥5280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Zatolmilast (BPN14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively.
Zatolmilast (BPN14770) displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2 IC50 = 127 nM).
BPN14770 is 17-fold less potent against mouse PDE4D7 (IC50 = 133 nM), binds to a primate-specific, N-terminal region of PDE4D.
BPN14770 elevates brain cAMP and facilitates hippocampal long-term potentiation (LTP) in wild-type and humanized PDE4D mice, improves cognitive performance, antagonized the amnesic effects of scopolamine and increased cAMP signaling in brain, and increased BDNF and markers of neuronal plasticity associated with memory.

物理化学性质&存储条件

分子量 405.801
分子式 C21H15ClF3NO2
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

2-(4-((2-(3-chlorophenyl)-6-(trifluoromethyl)pyridin-4-yl)methyl)phenyl)acetic acid

参考文献

1. Zhang C, et al. Neuropsychopharmacology. 2018 Oct;43(11):2299-2309.

2. Gurney ME, et al. Handb Exp Pharmacol. 2011;(204):167-92.

3. Gurney ME, et al. Sci Rep. 2017 Nov 7;7(1):14653.

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