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Nalfurafine hydrochloride
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。
Nalfurafine hydrochloride图片
CAS NO:152658-17-8
包装:5mg, 10mg
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
TRK-820 hydrochloride
产品介绍

生物活性

Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active kappa opioid receptor (KOR) agonist. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics. 

A single administration of subcutaneous TRK-820 significantly increased spontaneous ipsilateral rotational behavior of hemi-parkinsonian rats at 30 μg/kg though the efficacy is moderate and also significantly inhibited L-DOPA-induced dyskinesia at 10 and 30 μg/kg; this inhibition is reversed in the presence of nor-binaltorphimine, a kappa opioid receptor antagonist. TRK-820 dose-dependently inhibited phencyclidine-induced rat hyperlocomotion. TRK-820 dose-dependently attenuated the biochemical changes of both dopamine and serotonin in the prefrontal cortex of rats treated with phencyclidine without affecting their basal levels in normal rats.


化学数据

分子量513.03
分子式C28H33ClN2O5
CAS号152658-17-8
纯度>99%
溶解性(25°C)DMSO 30 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM1.9492 mL9.746 mL19.492 mL
5 mM0.3898 mL1.9492 mL3.8984 mL
10 mM0.1949 mL0.9746 mL1.9492 mL