Protopine

製品コードS3883 バッチS388301

化学情報

	Synonyms	Corydinine, Fumarine, Biflorine, Macleyine	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₁₉NO₅
	分子量	353.37	CAS No.	130-86-9
Solubility (25°C)*	体外	DMSO	30 mg/mL (84.89 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
in vitro	Protopine is found to be cytoprotective against oxidative stress-induced cell death in vitro. It inhibits several human CYP enzymes and is reported to be potent inhibitors of CYP2D6 and to suppress, albeit with less potency, the activities of CYP3A4, CYP1A2, and CYP2B6 as well. Protopine also inhibits CYP2C19^[1]. Protopine is a novel microtubule stabilizer with anticancer activity in HRPC cells through apoptotic pathway by modulating Cdk1 activity and Bcl-2 family of proteins^[2]. Protopine inhibits serotonin and noradrenaline transporter with IC50 values of 0.94 and 19.5 μM. The inhibiting effect of protopine on serotonin uptake (Ki = 0.92 μM) is stronger than that of protopine on NE uptake (Ki = 19.26 μM^[3].
in vivo	A pharmacokinetic study in rats after oral administration of a single dose of Rhizoma Corydalis Decumbentis extract, equivalent to 15.4 mg of protopine per kg of body weight, shows that the maximum plasma level of protopine reaches 348 ng/ml, i.e. 0.98 μM. In a similar study on rabbits, the maximum plasma concentration of protopine is 1.03 g/ml, i.e. 2.91 μM^[1]. Protopine may be a potential therapeuticagent of antidepressant which targeted on SERT and NET in mice models. It has an antidepressant-like effect on animal models^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HepG2 cells
	濃度	1-75 μM
	反応時間	24 h
	実験の流れ	The cells are grown in 75cm² flasks and sub-cultured before confluence. For all experiments, with the exception of gene reporter assays, HepG2 cells (passages 5–15) are seeded in the complete culture medium at a density of 1×10⁵ cells/cm2. After overnight stabilization, cells are treated with the tested alkaloids or 5 nM TCDD (positive control). Negative controls are treated with 0.1% (v/v) DMSO only.
動物実験	動物モデル	Male BALB/cj mice
	投薬量	5, 10, 20 mg/kg
	投与方法	i.p.

参考

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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