Nepicastat hydrochloride

Pricing Availability   Qty
说明: Potent and selective dopamine β-hydroxylase (DBH) inhibitor; orally bioavailable
化学名: 5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献 (1)
评论

生物活性 for Nepicastat hydrochloride

Nepicastat hydrochloride is a potent and selective dopamine β-hydroxylase (DBH) inhibitor (IC50 = 9 nM). Selective for DBH over 12 other enzymes. Decreases noradrenaline and increases dopamine levels in tissues and plasma in hypertensive rats. Prevents progressive left ventricular dysfunction in an in vivo heart failure model. Also potentiates the stimulus effects of cocaine without producing cocaine-like effects in rats. Orally bioavailable.

技术数据 for Nepicastat hydrochloride

分子量 331.81
公式 C14H15F2N3S.HCl
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 170151-24-3
PubChem ID 9840545
InChI Key DIPDUAJWNBEVOY-PPHPATTJSA-N
Smiles S=C(NC=C3CN)N3[C@H]2CCC1=C(F)C=C(F)C=C1C2.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Nepicastat hydrochloride

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 33.18 100

制备储备液 for Nepicastat hydrochloride

以下数据基于产品分子量 331.81。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 3.01 mL 15.07 mL 30.14 mL
5 mM 0.6 mL 3.01 mL 6.03 mL
10 mM 0.3 mL 1.51 mL 3.01 mL
50 mM 0.06 mL 0.3 mL 0.6 mL

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产品说明书 for Nepicastat hydrochloride

参考文献 for Nepicastat hydrochloride

参考文献是支持产品生物活性的出版物。

Manvich et al (2013) DA β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats. J.Pharmacol.Exp.Ther. 347 564 PMID: 24068832

Sabbah et al (2000) Effects of DA β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Circulation 102 1990 PMID: 11034950

Stanley et al (1997) Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of DA-beta-hydroxylase. Br.J.Pharmacol. 121 1803 PMID: 9283721


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关键词: Nepicastat hydrochloride, Nepicastat hydrochloride supplier, dopamine, beta-hydroxylase, inhibitors, inhibits, β, B-hydroxylase, DBH, noradrenaline, norepinephrine, potent, selective, orally, bioavailable, Hydroxylases, 5037, Tocris Bioscience

1 篇 Nepicastat hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Nepicastat hydrochloride 的部分引用包括:

Armando et al (2021) Synergistic Growth Inhibition of HT-29 Colon and MCF-7 Breast Cancer Cells with Simultaneous and Sequential Combinations of Antineoplastics and CNS Drugs. Int J Mol Sci 22 PMID: 34299028


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