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LY3020371 hydrochloride

LY3020371 hydrochloride

产品编号 T11911   CAS 1377615-44-5

LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.

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LY3020371 hydrochloride Chemical Structure
LY3020371 hydrochloride, CAS 1377615-44-5
规格 价格/CNY 货期 数量
2 mg ¥ 4,190 5日内发货
25 mg 待询 10-14周
50 mg 待询 10-14周
100 mg 待询 10-14周
其他形式的 LY3020371 hydrochloride:
产品目录号及名称: LY3020371 hydrochloride (T11911)
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参考文献
产品描述 LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.
靶点活性 mGluR3:2.5 nM (ki), mGluR2:5.3 nM (ki)
体外活性 LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC50=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC50=6.21 nM)[1]. LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM)[1].LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity (hmGlu2 Ki=5.26 nM;?hmGlu3 Ki=2.50 nM)[1].
体内活性 LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10?mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase[3].LY3020371 hydrochloride (Intravenous injection; 3-15 mg/kg) in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors[1].
分子量 395.81
分子式 C15H16ClF2NO5S
CAS No. 1377615-44-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Witkin JM, et al. In vitro pharmacological and rat pharmacokinetic characterization of LY3020371, a potent and selective mGlu2/3 receptor antagonist. Neuropharmacology. 2017 Mar 15;115:100-114. 2. Witkin JM, et al. Preclinical predictors that the orthosteric mGlu2/3 receptor antagonist LY3020371 will not engender ketamine-associated neurotoxic, motor, cognitive, subjective, or abuse-liability-related effects. Pharmacol Biochem Behav. 2017 Apr;155:43-55. 3. Wood CM, et al. Investigating the role of mGluR2 versus mGluR3 in antipsychotic-like effects, sleep-wake architecture and network oscillatory activity using novel Han Wistar rats lacking mGluR2 expression. Neuropharmacology. 2018 Sep 15;140:246-259.
Topiramate DL-AP3 TCN238 HBT1 LY339434 HCl ML337 LYPLAL1-IN-1 KM02894

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

LY3020371 hydrochloride 1377615-44-5 Neuroscience GluR LY-3020371 Hydrochloride LY 3020371 Hydrochloride LY-3020371 hydrochloride LY3020371 Hydrochloride Inhibitor inhibitor inhibit

 

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