(R)-Nepicastat HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(R)-Nepicastat HCl是有效的多巴胺β-羟化酶选择性抑制剂,对牛与人的IC50值分别为25.1 nM和18.3 nM[1].
多巴胺β-羟化酶参与调控小分子膜结合神经递质的合成.多巴胺β-羟化酶催化去甲肾上腺素合成[1].
(R)-Nepicastat HCl 是一种有效的和选择性的多巴胺β-羟化酶抑制剂,(R)-Nepicastat的作用较Nepicastat弱2 ~ 3倍[1].
在比格犬与自发性高血压大鼠中,Nepicastat剂量依赖性地减少大脑皮质\左心室以及动脉中去甲肾上腺素,并增加多巴胺以及多巴胺/去甲肾上腺素比率.在比格犬中,Nepicastat(2 mg/kg)显著减少血浆中去甲肾上腺素(52%),并增加多巴胺(646%)以及多巴胺/去甲肾上腺素比率[1].在毁脊髓的自发性高血压大鼠中,Nepicastat刺激交感节前神经,以抑制升压和正性变时作用.在自发性高血压大鼠中,Nepicastat(3 mg/kg)具有降压作用并降低肾血管阻力(38%)[2].在大鼠中,Nepicastat显著增加内侧前额叶皮质中Cocaine和Amphetamine诱导的胞外多巴胺积累.
参考文献：
[1]. Stanley WC, Li B, Bonhaus DW, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br J Pharmacol, 1997, 121(8): 1803-1809.
[2]. Stanley WC, Lee K, Johnson LG, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol, 1998, 31(6): 963-970.
[3]. Devoto P, Flore G, Saba P, et al. The dopamine beta-hydroxylase inhibitor nepicastat increases dopamine release and potentiates psychostimulant-induced dopamine release in the prefrontal cortex. Addict Biol, 2014, 19(4): 612-622.
| Storage | Store at -20°C |
| M.Wt | 331.81 |
| Cas No. | 195881-94-8 |
| Formula | C14H15F2N3S·HCl |
| Solubility | Soluble in DMSO |
| Chemical Name | 4-(aminomethyl)-3-[(2R)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1CC2=C(C=C(C=C2CC1N3C(=CNC3=S)CN)F)F.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
