VU0467154|1451993-15-9|-陌孚医药/Medlife

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VU0467154

目录号: PL06861 纯度: ≥99%

CAS No. :1451993-15-9

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中文名称	VU0467154
中文别名	5-氨基-3,4-二甲基-噻吩并[2,3-C]哒嗪-6-羧酸4-三氟甲磺酰基-苄基酰胺;化合物VU0467154
英文名称	VU0467154
英文别名	VU0467154;5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide;VU0467154, VU-0467154, VU 0467154;Thieno[2,3-c]pyridazine-6-carboxamide, 5-amino-3,4-dimethyl-N-[[4-[(trifluoromethyl)sulfonyl]phenyl]methyl]-;VUO467154 - M4 Receptor Agonist;VU0467154,Muscarinic acetylcholine receptor,VU 0467154,VU-0467154,mAChR,inhibit,Inhibitor
Cas No.	1451993-15-9
分子式	C₁₇H₁₅F₃N₄O₃S₂
分子量	444.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	VU0467154 是一种 M4 毒蕈碱的乙酰胆碱受体 (M4 muscarinic acetylcholine receptor (mAChR)) 的正向调节剂，能够增强小鼠，人和食蟹猴 M4 受体对乙酰胆碱的反应，pEC₅₀ 值分别为 7.75，6.2 和 6。
生物活性	VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC 50 s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
性状	Solid
IC50 & Target[1][2]	pEC50: of 7.75 (Rat M4 receptor), 6.2 (Human M4 receptor), 6 (Cynomolgus monkey M4 receptor)
体外研究(In Vitro)	VU0467154 is a positive allosteric modulators of the M4 muscarinic acetylcholine receptor (mAChR), robustly potentiates the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey (cyno) M4 receptor, respectively. VU0467154 does not potentiate the ACh response at rat and human M1, M2, M3, or M5. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	VU0467154 (1-56.6 mg/kg, p.o. or i.p.) reverses amphetamine-induced hyperlocomotion in rats. VU0467154 (0.3-30 mg/kg, i.p.) reverses amphetamine- and MK-801-induced hyperlocomotion in wild-type but not M4 KO mice. VU0467154 alone also enhances the acquisition of both contextual and cue-mediated fear conditioning in wild-type mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Bubser M, et al. Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42.

溶解度数据	In Vitro: DMSO : 13.89 mg/mL (31.25 mM; Need ultrasonic)配制储备液

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