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Dantrolene
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。
Dantrolene图片
CAS NO:7261-97-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
F 368
产品介绍
Dantrolene (F368) 是一种肌肉松弛剂,非竞争性地抑制人红细胞谷胱甘肽还原酶 (glutathione reductase),KiIC50值分别为 111.6 μM 和 52.3 μM。 Dantrolene 是一种兰尼碱受体拮抗剂和 Ca2+信号稳定剂。Dantrolene 可用于肌肉痉挛、恶性高热、亨廷顿病和其他神经阻滞剂恶性综合征的研究。
生物活性

Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyteglutathione reductase.KiandIC50values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome[1][2][3][4][5].

体外研究
(In Vitro)

Dantrolene interferes with calcium release from the sarcoplasmic reticulum and thus to inhibit excitation--contraction coupling[1].
Dantrolene acts directly on the RYR1 to reduce the extent of channel activation by calmodulin (CaM) and thereby decreases the Ca2+sensitivity of channel activation[2].
Dantrolene inhibits abnormal Ca2+release from the sarcoplasmic reticulum[3].
Dantrolene depresses excitation-contraction coupling in muscle fibers by inhibiting calcium release from the sarcoplasmic reticulum[3].
Dantrolene also shows calcium channel blocker effect in the smooth muscle membrane as well as antioxidative and cytoprotective properties[3].
Dantrolene affects the membrane calcium channel of smooth muscle cells and inhibits calcium influx[3].
Dantrolene is a skeletal muscle-specific muscle relaxant that works on the cardiac muscle. Dantrolene (0.3 μM) binds to domain 601-620 of RyR2 and corrects defective inter-domain interaction within RyR2 in failing hearts. This in turn inhibits spontaneous Ca2++ leak/Ca2+sparks, and improves cardiomyocyte function in failing hearts[4].

体内研究
(In Vivo)

Dantrolene is neuroprotective in Huntington's disease transgenic mouse model[5].
Feeding dantrolene (5 mg/kg) twice a week to YAC128 mice between 2 months and 11.5 months of age resulted in significantly improved performance in the beam-walking and gait-walking assays[5].

Animal Model:YAC128 transgenic mice (FVBN/NJ background strain) and WT mice[5]
Dosage:5 mg/kg
Administration:Fed orally twice per week from 2 to 11.5 months of age, followed by a washout period of 2 months (13.5 months of age)
Result:Resulted in significantly improved performance in the beam-walking and gait-walking assays.
Clinical Trial
分子量

314.25

性状

Solid

Formula

C14H10N4O5

CAS 号

7261-97-4

中文名称

丹曲洛林;丹曲林钠

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 20 mg/mL(63.64 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.1822 mL15.9109 mL31.8218 mL
5 mM0.6364 mL3.1822 mL6.3644 mL
10 mM0.3182 mL1.5911 mL3.1822 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。-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:
  • 1.

    Dantrolene is suspended in 50 μL of PBS with 2% corn flour[5].