DCPG - CAS:201730-11-2 - KKL Med Inc.

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DCPG (Synonyms:(S)-3,4-二甲酸苯基甘氨酸;(S)-3,4-Dicarboxyphenylglycine)

目录号 : KCM12385 CAS No. : 201730-11-2 纯度 : ≥95%

Data Sheet 产品使用指南

DCPG is a selective agonist of the class III metabotropic glutamate receptor 8 (mGluR8), with an EC value of 31 nM for inhibiting forskolin-stimulated cAMP formation in AV12-664 cells expressing human mGluR8. It is selective for mGluR8 over other mGluRs (ECs = >3.5 µM for mGluR1-7). In vitro, DCPG (1 μM) inhibits the responses of mouse retinal ganglion cells to the withdrawal of both bright and dim light stimuli by 68-69% relative to untreated cells. In vivo, DCPG (10 nmol, i.c.v.) reverses catalepsy induced by prolonged exposure to haloperidol in a rat model of Parkinson's disease.

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg	询价	In-stock

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生物活性

DCPG is a potent and selective mGlu8a receptor agonist with an EC50 of 31 nM for human mGlu8a. DCPG inhibits Forskolin stimulated cAMP formation by activating mGlu8, and modulates presynaptic glutamatergic transmission and synaptic plasticity. DCPG can be used in research on inflammatory pain, neuropathic pain, autism spectrum disorder, and glutamatergic synaptic plasticity.

IC₅₀&Target

hmGluR8a

31 nM (EC₅₀)

体外研究

DCPG (≤ 100 μM) selectively activates mGlu8a and inhibits forskolin stimulated cAMP formation in RGT (AV12-664) cells expressing human mGlu1-8. Its EC50 for mGlu8a is 31 nM, and for mGlu4a, mGlu6, and mGlu7a it is 8.8 μM, 3.6 μM, and>100 μM, respectively, indicating its selectivity for mGlu8a.
DCPG (0.5-400 μM; 5 min) inhibited the rapid component of dorsal root evoked ventral root potential (fDR-VRP) in neonatal rat spinal cord specimens, producing a biphasic concentration effect curve. The EC50 values of high affinity and low affinity components were 1.3 μM and 391 μM, respectively, with the high affinity component mainly mediated by mGlu8.

体内研究

DCPG (10, 30, or 60 mg/kg; 15 minutes before formal; i. In a male Swiss Webster mouse formalized inflammatory pain model, dose-dependent reduction of early and late nociceptive responses was observed, with the effect of 60 mg/kg being blocked by the PAG Group III metabolomic glutamate receptor antagonist MSOP.
DCPG (30 or 60 mg/kg; Carrageenan for the first 15 minutes; i. P.) In the carrageenan inflammatory pain model, there was an increase in the latent period of thermal and mechanical foot contractions, while administration of DCPG 1 hour after carrageenan had no significant effect.

DCPG (60 mg/kg; single dose; i.p.) increased the latency of thermal and mechanical foot contractions on the third day after chronic sciatic nerve compression injury, thereby reducing thermal hyperalgesia and mechanical allodynia, but had no significant effect on the seventh day after injury.
DCPG (1 μM/0.5 μL per side; intra DG) reversed the decreased Social Novelty Preference Index (SNPI) and enhanced fEPSP LTP of the VPA exposed rat PP-DG pathway in a pre-existing VPA induced Wistar rat autism model, while inhibiting LTP in normal control rats.

Animal Model:	Male Swiss-Webster mice, formalin-induced pain model
Dosage:	10, 30, 60 mg/kg; 15 min before formalin
Administration:	i.p.; single dose
Result:	Dose-dependently decreased early and late nociceptive behaviors; the effect of 60 mg/kg was blocked by intra-PAG MSOP.

Animal Model:	Male Swiss-Webster mice, formalin-induced pain model
Dosage:	10, 30, 60 mg/kg; 15 min before formalin
Administration:	i.p.; single dose
Result:	Dose-dependently decreased the late hyperalgesic phase.

Animal Model:	Male Swiss-Webster mice, carrageenan-induced inflammatory pain model
Dosage:	30, 60 mg/kg; 15 min before carrageenan
Administration:	i.p.; single dose
Result:	Increased thermal withdrawal latency and mechanical withdrawal threshold; the 60 mg/kg effect was blocked by intra-PAG MSOP.

分子式

C₁₀H₉NO₆

分子量

239.18

CAS号

201730-11-2

中文名称

(S)-3,4-二甲酸苯基甘氨酸

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: 20 mg/mL (83.62 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.1810 mL	20.9048 mL	41.8095 mL
5 mM	0.8362 mL	4.1810 mL	8.3619 mL
10 mM	0.4181 mL	2.0905 mL	4.1810 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。-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。

纯度： ≥95%

Data Sheet

产品使用指南

Gholipour P, et al. Effects of (S)-3,4-DCPG, an mGlu8 receptor agonist, on hippocampal long-term potentiation at perforant pathway-dentate gyrus synapses in prenatal valproic acid-induced rat model of autism. Scientific reports. 2024 Jun 07;14(1):13168.

The molarity calculator equation

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

质量

浓度

体积

分子量*

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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

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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

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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

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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