货号	规格	价格	上海	北京	珠海	重庆	武汉
S89696-5mg促销	99.70%	￥550.00 ￥440.00 S89696-5mg ￥440.00 现货	7 7	-	-	-	-
S89696-10mg促销	99.70%	￥970.00 ￥776.00 S89696-10mg ￥776.00 现货	5 5	-	-	-	-
S89696-25mg促销	≥98%	￥1910.00 ￥1520.00 S89696-25mg ￥1520.00 2-3天	0 货期：2-3天	-	-	-	-
S89696-100mg	≥98%	￥3920.00 S89696-100mg ￥3920.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia

靶点：

mAChR;AChR

体外研究：

Application of M1 PAM VU0453595 (3 μM) induces a transient increase in excitability of medium spiny neurons (MSNs).

体内研究：

VU0453595 potentiates M1-mediated muscarinic long-term depression (mLTD). VU0453595 (1-10 mg/kg; i.p.) reverses behavioral deficits induced by repeated phencyclidine (PCP) administration. Animal Model: Male C57BL6/J mice (8-9 weeks old) Dosage: 1, 3, or 10 mg/kg Administration: Intraperitoneal (i.p.); 10 mL/kg; administered 30 min before the social interaction test Result: Rescued deficits in social interaction observed in PCP-treated mice.

参考文献：

1. A Ghoshal, et al. Potentiation of M1 Muscarinic Receptor Reverses Plasticity Deficits and Negative and Cognitive Symptoms in a Schizophrenia Mouse Model. Neuropsychopharmacology. 2016 Jan;41(2):598-610.

2. Sean P Moran, et al. M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771.

3. Xiaohui Lv, et al. M1 muscarinic activation induces long-lasting increase in intrinsic excitability of striatal projection neurons. Neuropharmacology. 2017 May 15;118:209-222.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.102 ml	15.512 ml	31.023 ml
5 mM	0.62 ml	3.102 ml	6.205 ml
10 mM	0.31 ml	1.551 ml	3.102 ml
50 mM	0.062 ml	0.31 ml	0.62 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

VU0453595

6-[[2-Fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)