1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. Dipraglurant

Dipraglurant  (Synonyms: ADX48621)

目录号: HY-14859 纯度: 99.90%
COA 产品使用指南

Dipraglurant (ADX48621) 是一种有效的,选择性的,具有口服活性和可透过血脑屏障的 mGluR5 的负变构调节剂 (NAM),IC50 值为 21 nM。Dipraglurant 可以减少左旋多巴诱发的运动障碍 (LID)。

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Dipraglurant Chemical Structure

Dipraglurant Chemical Structure

CAS No. : 872363-17-2

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4085
In-stock
1 mg ¥1400
In-stock
5 mg ¥3190
In-stock
10 mg ¥4400
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100 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo[1][2]. Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

mGluR5

21 nM (IC50)

体外研究
(In Vitro)

Dipraglurant (1-10 μM; 15 min) counteracts the abnormal membrane responses and calcium rise induced either by the D2R agonist quinpirole or by caged dopamine (NPEC-Dopamine)[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Dipraglurant (3-30 mg/kg; a single p.o.) reduces L-dopa-induced chorea and dystonia and does not interfere with the efficacy of L-dopa in treating parkinsonian disability macaque[1].
Dipraglurant exhibits Cmax (1.040, 1.380, 5.310 ng/mL) Tmax (1.0, 0.5, 1.0 h) and AUCinf (2.230, 2.860, 15.700) following p.o. administration (3, 10, 30 mg/kg) in macaque[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

265.29

Formula

C16H12FN3

CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 40 mg/mL (150.78 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7695 mL 18.8473 mL 37.6946 mL
5 mM 0.7539 mL 3.7695 mL 7.5389 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.90%

参考文献

Dipraglurant 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7695 mL 18.8473 mL 37.6946 mL 94.2365 mL
5 mM 0.7539 mL 3.7695 mL 7.5389 mL 18.8473 mL
10 mM 0.3769 mL 1.8847 mL 3.7695 mL 9.4236 mL
15 mM 0.2513 mL 1.2565 mL 2.5130 mL 6.2824 mL
20 mM 0.1885 mL 0.9424 mL 1.8847 mL 4.7118 mL
25 mM 0.1508 mL 0.7539 mL 1.5078 mL 3.7695 mL
30 mM 0.1256 mL 0.6282 mL 1.2565 mL 3.1412 mL
40 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3559 mL
50 mM 0.0754 mL 0.3769 mL 0.7539 mL 1.8847 mL
60 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5706 mL
80 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1780 mL
100 mM 0.0377 mL 0.1885 mL 0.3769 mL 0.9424 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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目录号:
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