GlpBio

FITM

目录号: GC34081纯度: >98.00%同义词: 4-氟-N-[4-[6-(异丙基氨基)嘧啶-4-基]-1,3-噻唑-2-基]-N-甲基苯甲酰胺
An antagonist of mGluR1
FITM
Cas No.: 932737-65-0
规格价格库存数量操作
1mg¥319.00现货
1
5mg¥720.00现货
1
10mg¥1,080.00现货
1
25mg¥2,160.00现货
1
50mg¥3,240.00现货
1
100mg¥4,770.00现货
1
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产品描述 Description

FITM is an antagonist of metabotropic glutamate receptor 1 (mGluR1; IC50 = 5.1 nM for the human receptor).1 It is selective for mGluR1 over mGluR2, mGluR5, and mGluR8 (IC50s = >10, 7, and >10 ?M, respectively). FITM (0.3 mg/kg) decreases methamphetamine-induced hyperlocomotion in mice and reverses disruptions in prepulse inhibition induced by methamphetamine and ketamine in rats when administered at a dose of 1 mg/kg.

1.Satoh, A., Nagatomi, Y., Hirata, Y., et al.Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonistBioorg. Med. Chem. Lett.19(18)5464-5468(2009)

实验参考方法 Experimental Reference Method

Animal experiment:

Rats: Sprague–Dawley rats are treated with different doses of unlabeled FITM (0, 1, 5, or 30 μg/kg or 1 mg/kg) just before a bolus injection of 18F-FITM (17–18 MBq, 30–40 pmol, 0.1 mL). Estimations of equilibrium state and BPND were acquired[3].

References:

[1]. Wu H, et al. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science. 2014 Apr 4;344(6179):58-64.
[2]. Bai Q, et al. Investigation of allosteric modulation mechanism of metabotropic glutamate receptor 1 by molecular dynamics simulations, free energy and weak interaction analysis. Sci Rep. 2016 Feb 18;6:21763.
[3]. Yamasaki T, et al. In vivo measurement of the affinity and density of metabotropic glutamate receptor subtype 1 in rat brain using 18F-FITM in small-animal PET. J Nucl Med. 2012 Oct;53(10):1601-7.
[4]. Xie L, et al. Molecular imaging of ectopic metabotropic glutamate 1 receptor in melanoma with a positron emission tomography radioprobe (18) F-FITM. Int J Cancer. 2014 Oct 15;135(8):1852-9.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
932737-65-0
同义词
4-氟-N-[4-[6-(异丙基氨基)嘧啶-4-基]-1,3-噻唑-2-基]-N-甲基苯甲酰胺
SMILES
O=C(N(C)C1=NC(C2=NC=NC(NC(C)C)=C2)=CS1)C3=CC=C(F)C=C3
分子式
C18H18FN5OS
分子量
371.43 g/mol
溶解性
DMSO : ≥ 150 mg/mL (403.84 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol