Dipraglurant (Synonyms:ADX48621)
目录号 : KM10887 CAS No. : 872363-17-2 纯度 : 98%

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)。

规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg 询价 In-stock
200mg 询价 In-stock

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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.

体外研究

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).

体内研究

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.
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.

分子式
C16H12N3F
分子量
265.29
CAS号
872363-17-2
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 : ≥ 40 mg/mL (150.78 mM)

* "≥" 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
10 mM 0.3769 mL 1.8847 mL 3.7695 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。

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