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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Monoamine Transporter-D-578
D-578

Chemical Structure : D-578

CAS No.: 2454461-06-2

D-578 (D578)

货号: PC-21114Not For Human Use, Lab Use Only.

D-578 is a potent, orally active triple monoamine reuptake inhibitor with Ki values of 16.2. 16.2, 3.23 nM, and 29.6, 20.6, 6.10 nM for the rat brain and cloned human dopamine, serotonin and norepinephrine transporters, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

D-578 is a potent, orally active triple monoamine reuptake inhibitor with Ki values of 16.2. 16.2, 3.23 nM, and 29.6, 20.6, 6.10 nM for the rat brain and cloned human dopamine, serotonin and norepinephrine transporters, respectively.
D-578 has moderate affinity for 5HT2c (Ki = 73 nM) and very weak affinity for 5HT2b (Ki = 425 nM), does not display appreciable affinity for other brain targets.
D-578 (10 mg/kg) shows efficacy in normalizing traumatic stress-induced extinction-retention learning in a fear conditioning SPS animal PTSD model experiment.
D-578 is far more efficacious than paroxetine (Cat# PC-46649), an SSRI currently used for treatment of PTSD.

物理化学性质&存储条件

分子量 481.56
分子式 C26H25F2N3O2S
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

(2S,4R,5R)-5-(((2-aminobenzo[d]thiazol-6-yl)methyl)amino)-2-(bis(4-fluorophenyl)methyl)tetrahydro-2H-pyran-4-ol

参考文献

1. Aloke K Dutta, et al. Eur J Pharmacol. 2019 Nov 5;862:172632.

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