5,7-Dichlorokynurenic Acid - CAS:131123-76-7

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5,7-Dichlorokynurenic Acid (Synonyms:5,7-二氯犬尿喹啉酸;5,7-DCKA)

目录号 : KCM10999 CAS No. : 131123-76-7 纯度 : ≥98%

Data Sheet 产品使用指南

5,7-Dichlorokyneurenic acid (5,7-DCKA) is a derivative of kynurenic acid and an NMDA receptor antagonist (K = 40 nM in a radioligand binding assay). It selectively inhibits glycine- over kainate-induced NMDA currents at 15 μM in Xenopus oocytes expressing rat NMDA receptors. 5,7-DCKA reduces NMDA-induced neurotoxicity in primary rat cortical neurons by 55 to 90% when used at concentrations ranging from 1 to 10 μM. In vivo, 5,7-DCKA (0.97-97 nmol) reverses mechanical hyperalgesia in magnesium-deficient rats in a dose-dependent manner. It blocks the positive ionotropic effect, hypertension, and increase in myocardial oxygen demand induced by electrical stimulation of the paraventricular nucleus (PVN) in anesthetized rabbits. 5,7-DCKA also increases social interaction time in the social interaction test and time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, as well as disinhibits conflict responding in the Cook and Davidson conditioned conflict paradigm.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

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生物活性

5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission.

IC₅₀&Target

NMDA Receptor

体外研究

5,7-dichlorokynurenic acid (0.2-400 μM) is a potent competitive antagonist of the glycine site of NMDA receptors expressed in Xenopus oocytes injected with rat brain mRNA, with a KB value of 65 nM, exhibiting 509-fold higher selectivity for this site compared to the kainate receptor [1].

5,7-dichlorokynurenic acid (40 nM–10 μM; 60 min on ice) effectively displaced [3H]glycine bound to the strychnine-insensitive glycine site on rat cortical membranes, with a Ki of 40 nM; and did not bind to the NMDA recognition site at 10 μM [1].

5,7-Dichlorokynurenic acid (1-10 μM) can mitigate NMDA-induced neuronal damage in primary rat cortical cell cultures, with 1 μM providing 55-79% protection and 10 μM yielding 62-90% protection [1].

体内研究

5,7-Dichlorokynurenic acid (30.0-100.0 mg/kg; intraperitoneal injection; single dose) can produce anxiolytic-like effects in the social interaction model, increasing social interaction time by 37% at a dose of 30.0 mg/kg and by 32% at 100.0 mg/kg, with the highest dose leading to reduced motor activity [2].
5,7-Dichlorokynurenic acid (100.0 mg/kg; intraperitoneal injection; single dose) exhibited anxiolytic-like effects in the elevated plus maze model, increasing open arm exploration time by 41% at the 100.0 mg/kg dose while reducing spontaneous activity [2].
5,7-Dichlorokynurenic acid (100.0-173.0 mg/kg; intraperitoneal injection; single dose) can reverse the suppressed conflict response in the Cook and Davidson conditional anxiety model at doses of 100.0 mg/kg and 173.0 mg/kg without altering unconditioned responses [2].
5,7-Dichlorokynurenic acid (intraperitoneal injection; single dose, 10.0-100.0 mg/kg) did not generalize the discriminative stimulus of MK-801 at a dose of 10.0 mg/kg, while at 100.0 mg/kg, only one out of four rats exhibited extremely weak partial generalization [2].

Animal Model:	Wistar rats (male, 200-300 g)
Dosage:	30.0 mg/kg; 100.0 mg/kg
Administration:	i.p.; single dose
Result:	Increased social interaction time significantly by +37% with no significant change in motor activity at 30.0 mg/kg. Increased social interaction time significantly by +32%, and decreased motor activity significantly by -34% at 100.0 mg/kg.

分子式

C₁₀H₅Cl₂NO₃

分子量

258.06

CAS号

131123-76-7

中文名称

5,7-二氯犬尿喹啉酸;[3-(三氟甲基)吡啶]甲烷磺酰氯;5,7-二氯-4-羟基-2-喹啉甲酸钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°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 : 25 mg/mL (96.88 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8751 mL	19.3753 mL	38.7507 mL
5 mM	0.7750 mL	3.8751 mL	7.7501 mL
10 mM	0.3875 mL	1.9375 mL	3.8751 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

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 (9.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.69 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。
2.

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

Solubility: ≥ 2.5 mg/mL (9.69 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.69 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。

纯度： ≥98%

Data Sheet

产品使用指南

[1]. McNamara D, et al. 5,7-Dichlorokynurenic acid, a potent and selective competitive antagonist of the glycine site on NMDA receptors. Neurosci Lett. 1990;120(1):17-20.

[2]. Corbett R, et al. Effects of 5,7 dichlorokynurenic acid on conflict, social interaction and plus maze behaviors. Neuropharmacology. 1993;32(5):461-466.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器