FPTQ

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FPTQ

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

864863-72-9

FPTQ 是一种有效的mGluR₁拮抗剂，抑制人和鼠的IC₅₀值分别为 6 nM 和 1.4 nM。FPTQ 具有抗氧化、抗炎作用。

生物活性

FPTQ is potentmGluR₁antagonist withIC₅₀values of 6 nM and 1.4 nM for human and mousemGluR1respectively^[1]. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo^[2].

IC₅₀& Target^[1]

Human mGluR1

6 nM (IC₅₀)

Mouse mGluR1

1.4 nM (IC₅₀)

体外研究
(In Vitro)

FPTQ (0.5-10 μM) does not shows any cytotoxicity was not observed at 0.5, 1, 5, and 10 μM in RAW264.7 macrophage cells^[2].
FPTQ (1-20 μM; 24 hours) reduces LPS-induced NO production at >1 μM FPTQ, and at 10 μM, FPTQ treatment causes a 31% anti-oxidant effect in RAW264.7 macrophage cells^[2].
FPTQ (1-20 μM; 24 hours) dramaticly decreases LPS-induced expression levels of IL-1β and Il-6. At a concentration of 10 μM, FPTQ causes a 27% and 44% reduction in the mRNA expression of IL-1β and Il-6, respectively in RAW264.7 macrophage cells^[2].

RT-PCR^[1]

Cell Line:	RAW264.7 macrophage cells
Concentration:	1, 10, or 20 μM
Incubation Time:	24 hours
Result:	Decreased IL-1β and IL-6 mRNA expression

体内研究
(In Vivo)

FPTQ (5-20 μM) decreases the number of neutrophils migrating to the amputation site in zebrafish larvae by tail amputation. In the tailfin wound method, the number of neutrophils collecting at the wound site also decreases in a dose-dependent manner in zebrafish^[2].
In a LPS-induced inflammation zebrafish model, LPS solution is injected into the yolks of Tg(mpx:EGFP)ⁱ¹¹⁴zebrafish larvae and exposed the zebrafish larvae immediately to FPTQ treatment.
FPTQ (20 μM; 4 hours) significantly decreases the fluorescent neutrophils after yolk injection and has an anti-inflammatory effect during the early phase of inflammation^[2].

分子量

305.31

性状

Solid

Formula

C₁₇H₁₂FN₅

CAS 号

864863-72-9

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
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL(109.17 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.2754 mL	16.3768 mL	32.7536 mL
5 mM	0.6551 mL	3.2754 mL	6.5507 mL
10 mM	0.3275 mL	1.6377 mL	3.2754 mL

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.19 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在本网站选购。