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Kynurenic acid sodium
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。
Kynurenic acid sodium图片
CAS NO:2439-02-3

Kynurenic acid sodium 是一种内源性色氨酸代谢物,是针对靶点NMDA, glutamate, α7 nicotinic acetylcholine receptor的光谱性拮抗剂。Kynurenic acid sodium 也是GPR35/CXCR8的激动剂。
生物活性

Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targetingNMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist ofGPR35/CXCR8.

IC50& Target

NMDA Receptor

 

Human Endogenous Metabolite

 

体外研究
(In Vitro)

GPR35 functions as a receptor for the kynurenine pathway intermediate kynurenic acid. Kynurenic acid elicits calcium mobilization and inositol phosphate production in a GPR35-dependent manner in the presence of Gqi/ochimeric G proteins. Kynurenic acid stimulates [35S]guanosine 5′-O-(3-thiotriphosphate) binding in GPR35-expressing cells, an effect abolished by pertussis toxin treatment. Kynurenic acid also induces the internalization of GPR35[1]. KYNA’s neuroinhibitory qualities and its neuroprotective and anticonvulsant effects are discovered using concentrations of the compound in the millimolar range. This, as well as the low affinity of KYNA at each of the three ionotropic glutamate receptors responsible for these effects [NMDA, alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) and kainate], together with the realization that KYNA concentrations in the mammalian brain are in the sub-micromolar range, suggested that other receptors might serve as targets of endogenous Kynurenic acid. Kynurenic acid, with a shallower inhibition curve and non-competitively, antagonizes α7nAChRs on cultured hippocampal neurons with an IC50in the low micromolar range[2].

体内研究
(In Vivo)

Kynurenic acid affects the activity of leukocytes in the peripheral blood of mice, although the lowest one (2.5 mg/L) has the most profound influence in contrast to the highest one (250 mg/L), which produces the weakest effect. The lowest Kynurenic acid dose stimulates the proliferative response of T lymphocytes (p<0.05), after 7 and 28 days of administering the acid to the animals[3].

Clinical Trial
分子量

211.15

性状

Solid

Formula

C10H6NNaO3

CAS 号

2439-02-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 50 mg/mL(236.80 mM;Need ultrasonic)

H2O : 0.1 mg/mL(0.47 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.7360 mL23.6798 mL47.3597 mL
5 mM0.9472 mL4.7360 mL9.4719 mL
10 mM0.4736 mL2.3680 mL4.7360 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 (sealed storage, away from moisture)。-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 (11.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.84 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
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (11.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.84 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (11.84 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (11.84 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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