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SNAP 94847

SNAP 94847

产品编号 T5406   CAS 487051-12-7
别名: SNAP-94847

SNAP 94847 (SNAP-94847) 是一种选择性黑色素浓缩激素受体1 拮抗剂,Ki 为 2.2 nM。它具有抗焦虑和抗抑郁活性,可减少小鼠的食物摄入。 在相同实验条件下,摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性,但盐形式 SNAP 94847 hydrochloride 的水溶性和稳定性通常比游离态更好。

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SNAP 94847 Chemical Structure
SNAP 94847, CAS 487051-12-7
规格 价格/CNY 货期 数量
25 mg ¥ 5,130 6-8周
50 mg ¥ 6,670 6-8周
1 mL * 10 mM (in DMSO) ¥ 1,870 6-8周

SNAP 94847 的其他形式现货产品:

SNAP 94847 hydrochloride
其他形式的 SNAP 94847:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: SNAP 94847 (T5406)
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参考文献
产品描述 SNAP 94847 (SNAP-94847) is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake in mice.
靶点活性 MCH1 receptor:2.2 nM (Ki, cell free)
体外活性 SNAP-94847 showed a favorable combination of MCH1 receptor affinity (Ki: 2.2 nM) and human R1A receptor (>80-fold) and D2 (>500-fold) selectivity [1].
体内活性 SNAP-94847 (10 mg/kg, p.o.) had no effect on basal water consumption measured over 2 h: vehicle-treated (2.0 mL); 16g-treated (2.3 mL). MCH-evoked water intake was inhibited significantly by SNAP-94847 at doses of 1.0, 2.5, and 10 mg/kg [1]. BALB/c mice treated for 21 days with fluoxetine or SNAP 94847 (20 mg/kg/day) showed marked increases in quinpirole-induced locomotor activity, with the onset of hyper-locomotion appearing earlier in the time course after SNAP 94847 compared to fluoxetine. Administration of either compound for 7 days was also sufficient to augment the quinpirole response in BALB/c mice [2]. The intra-locus coeruleus and intracerebroventricular injections of melanin-concentrating hormone and chronic injections of corticosterone increased immobility time in the forced swim test and decreased sucrose preference in the sucrose preference test. All these depressive-like behaviors were reversed by an intra-locus coeruleus microinjection of SNAP-94847 [3].
动物实验 Chronically treated Sprague–Dawley rats were administered fluoxetine (18 mg/kg/day) or SNAP 94847 (20 mg/kg/day) via oral gavage in 20% beta-cyclodextrin for 2 weeks (1 injection, 6 h into light cycle). For acute treatment, drugs were given orally in 20% betacyclodextrin 1 h before testing. On each test day, locomotor activity was recorded during a 60 min habituation to the novel locomotor cage, after which the rats were administered quinpirole (0.3 mg/kg, i.p.) and returned immediately to the cage, where locomotor activity was measured for an additional 180 min. In each case-control animals were administered the corresponding vehicle, without drug [2].
别名 SNAP-94847
分子量 478.57
分子式 C29H32F2N2O2
CAS No. 487051-12-7

存储

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

溶解度

DMSO: 20 mg/mL (41.79 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0896 mL 10.4478 mL 20.8956 mL 52.239 mL
5 mM 0.4179 mL 2.0896 mL 4.1791 mL 10.4478 mL
10 mM 0.209 mL 1.0448 mL 2.0896 mL 5.2239 mL
20 mM 0.1045 mL 0.5224 mL 1.0448 mL 2.6119 mL

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TargetMol Library Books参考文献

1. Chen CA, et al. Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits. J Med Chem. 2007 Aug 9;50(16):3883-90. 2. Marsteller DA, et al. The MCH1 receptor antagonist SNAP 94847 induces sensitivity to dopamine D2/D3 receptor agonists in rats and mice. Eur J Pharmacol. 2009 Jan 5;602(1):66-72. 3. Ye H, et al. Melanin-Concentrating Hormone (MCH) and MCH-R1 in the Locus Coeruleus May Be Involved in the Regulation of Depressive-Like Behavior. Int J Neuropsychopharmacol. 2018 Dec 1;21(12):1128-1137.
MS21570 IBC 293 Urotensin II, mouse TFA (9047-55-6 free base) FL104 LY2922470 Lodoxamide (+/-)-Pinocembrin PW0787

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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

SNAP 94847 487051-12-7 Endocrinology/Hormones GPCR/G Protein GPR Melanin-concentrating Hormone Receptor (MCHR) inhibit Antidepressant SNAP-94847 MCHR1 (GPR24) Melanin concentrating hormone receptor 1 Inhibitor SNAP94847 anxiolytic anxiety inhibitor

 

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