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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-NLX-101
NLX-101

Chemical Structure : NLX-101

CAS No.: 635323-95-4

NLX-101 (F15599)

货号: PC-73308Not For Human Use, Lab Use Only.

NLX-101 (F15599) is a potent, highly selective post-synaptic 5-HT1A receptor agonist with Ki of 3.4 nM.

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10 mg ¥2980 In stock
25 mg ¥4980 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

NLX-101 (F15599) is a potent, highly selective post-synaptic 5-HT1A receptor agonist with Ki of 3.4 nM.
NLX-101 (F15599) is over 1000-fold selective with respect to the other 5-HT1 receptor subtypes, 5-HT2-7 receptor families, and also numerous GPCRs, transporters, ion channels, and enzymes.
NLX-101 (F15599) activates h5-HT1A receptors with an efficacy superior to that of the prototypical 5-HT1A agonist (+/-)-8-OH-DPAT in cellular model of signal transduction.
NLX-101 (F15599), unlike 5-HT, more potently and efficaciously stimulated G(αi) than G(αo) activation.
NLX-101 (F15599) potently activated ERK1/2 phosphorylation and strongly induced c-fos mRNA expression in rat prefrontal cortex.
NLX-101 (F15599) attenuates muscular hyperalgesia in reserpine-induced myalgia model.

物理化学性质&存储条件

分子量 394.85
分子式 C19H21ClF2N4O
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

(3-Chloro-4-fluorophenyl)[4-fluoro-4-[[[(5-methyl-2-pyrimidinyl)methyl]amino]methyl]-1-piperidinyl]methanone

参考文献

1. Maurel JL, et al. J Med Chem. 2007 Oct 4;50(20):5024-33.

2. Newman-Tancredi A, et al. Br J Pharmacol. 2009 Jan;156(2):338-53.

3. Assié MB, et al. Int J Neuropsychopharmacol. 2010 Nov;13(10):1285-98.

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