Nepicastat (SYN-117) 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.
Nepicastat(SYN-117)HCl是一种强效的和选择性的多巴胺β-羟化酶抑制剂,在牛和人体中IC50值分别为8.5 nM和 9 nM [ 1 ] 。
多巴胺-β-羟化酶是一种参与小分子膜结合神经递质合成的酶。多巴胺-β-羟化酶催化去甲肾上腺素的合成[ 1 ]。
Nepicastat(SYN-117)HCl是一种强效的和选择性的多巴胺β-羟化酶抑制剂。(R)-Nepicastat的效力比Nepicastat 小2-3 倍[ 1 ]。
在比格犬和自发性高血压大鼠中,Nepicastat剂量依赖性地减少去甲肾上腺素,增加大脑皮层、左心室和动脉中多巴胺和多巴胺/去甲肾上腺素比率。在比格犬中,Nepicastat(2 mg/kg)显著地减少52%的去甲肾上腺素,并增加646%的多巴胺及血浆中的多巴宁/去甲肾上腺素比率[1]。在毁脊髓自发性高血压大鼠中,Nepicastat抑制由节前交感神经刺激导致的血压升高和正性变时作用。在自发性高血压大鼠中,Nepicastat(3 mg/kg)表现出抗高血压作用并降低38%的肾血管阻力[ 2 ]。在大鼠中,Nepicastat显著地增加内侧前额叶皮层中可卡因和苯丙胺诱导的细胞外多巴胺积累[ 3 ]。
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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 331.81 |
Cas No. | 170151-24-3 |
Formula | C14H15F2N3S·HCl |
Solubility | insoluble in H2O; insoluble in EtOH; ≥16.6 mg/mL in DMSO |
Chemical Name | 4-(aminomethyl)-3-[(2S)-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。 |
描述 | Nepicastat是一种强效的和选择性的牛和人体多巴胺β-羟化酶抑制剂,IC50值分别为8.5 nM和9 nM。 | |||||
靶点 | bovine dopamine-β-hydroxylase | human dopamine-β-hydroxylase | ||||
IC50 | 8.5 nM | 9 nM |
质量控制和MSDS
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