Nilvadipine (75530-68-6) is a novel DHP L-type Ca2+ channel blocker that also inhibits Syk.1 Blocks Aβ production, APPβ secretion and reduces BACE-1 expression in CHO cells over-expressing Aβ in vitro. Enhances clearance of Aβ across the blood brain barrier in vivo. Reduces brain Aβ levels in a mouse tauopathy model.1 Clinically useful antihypertensive agent.2 Has been shown to prevent cognitive decline in some clinical trials.3 Nilvadipine produces a protective effect on glutamate neurotoxicity in retinal ganglion cells, an effect not shared by other L-type Ca2+ channel blockers such as nifedipine and diltiazem.4 Syk抑制剂/钙通道阻滞剂nilvadipine(75530-68-6)是一种新型DHP l型Ca2+通道阻滞剂,也可抑制Syk.1,阻断a β的产生,APPβ的分泌,降低体外过表达a β的CHO细胞的BACE-1表达。 增强体内血脑屏障对Aβ的清除。 降低小鼠tauopathy模型的脑a β水平 临床有用的降压药 在一些临床试验中被证明可以防止认知能力下降 Nilvadipine对视网膜神经节细胞中的谷氨酸神经毒性有保护作用,这是其他l型Ca2+通道阻滞剂如硝苯地平和地尔硫卓所不具有的作用 。
References/Citations:
1) Paris et al. (2014), The spleen tyrosine kinase (Syk) regulates Alzheimer amyloid-β production and Tau hyperphosphorylation; J. Biol. Chem., 289 33927 2) Rosenthal (1994), Nilvadipine: profile of a new calcium antagonist. An overview; J. Cardiovasc. Pharmacol. 24 Suppl 2 S92 3) Nimmrich and Eckert (2013), Calcium channel blockers and dementia; Br. J. Pharmacol. 169 1203 4) Otori et al. (2003), Protective effect of nilvadipine against glutamate neurotoxicity in purified retinal ganglion cells; Brain Res. 961 213
CAS:
75530-68-6
Catalog Number:
10-3035
Activity:
Syk inhibitor and Calcium channel blocker
Chemical Name:
2-Cyano-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 3-methyl 5-(1-methylethyl) ester
Alternate Names:
FR34235
Molecular Weight:
385.38
Molecular Formula:
C19H19N3O6 Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml).
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
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