Cilnidipine

製品コードS1293 バッチS129302

印刷

化学情報

 Chemical Structure Synonyms FRC-8653 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C27H28N2O7

分子量 492.52 CAS No. 132203-70-4
Solubility (25°C)* 体外 DMSO 99 mg/mL (201.0 mM)
Ethanol 15 mg/mL (30.45 mM)
Water Insoluble
* <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 Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.
in vitro Cilnidipine (10 mM) suppresses the elevation of the ratio induced by 40 mM KCl, and this suppression is effectively inhibited after the treatment with omega-conotoxin GVIA.[1]
in vivo Cilnidipine reduces Ca(2+) influx via N-type Ca(2+) channels after NMDA receptors activation and then protects neurons against ischemia-reperfusion injury in the rat retina in vivo. [2] Cilnidipine significantly prevents the increase in desmin staining and restores the glomerular podocin and nephrin expression compared with amlodipine in spontaneously hypertensive rat/ND mcr-cp (SHR/ND). Cilnidipine also prevents the increase in renal angiotensin II content, the expression and membrane translocation of NADPH oxidase subunits and dihydroethidium staining in SHR/ND. [3] Cilnidipine (30 mg/kg/d as food admix) treatment suppresses the increase in systolic blood pressure in Dahl salt-sensitive rats. Cilnidipine inhibits the increase in blood urea nitrogen and decrease in creatinine clearance as well as progression of glomerular sclerosis. Cilnidipine reduces plasma norepinephrine level and plasma rennin activity compared with vehicle-treated Dahl S rats. [4] Cilnidipine suppresses the pressor response induced by sympathetic nerve stimulation and angiotensin II in pithed rats. Cilnidipine or omega-conotoxin MVIIA decreases mean blood pressure, but slightly increases heart rate in anesthetized rats. Cilnidipine can affect sympathetic N-type Ca(2+) channels in addition to vascular L-type Ca(2+) channels in antihypertensive doses in the rat in vivo. [5]

プロトコル(参考用のみ)

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Calcium channel blocker amlodipine besylate therapy is associated with reduced case fatality rate of COVID-19 patients with hypertension [ Cell Discov, 2020, 6(1):96] PubMed: 33349633
A Patient-Derived Cell Atlas Informs Precision Targeting of Glioblastoma [ Cell Rep, 2020, 32(2):107897] PubMed: 32668248
High-Throughput Screening of an FDA-Approved Drug Library Identifies Inhibitors against Arenaviruses and SARS-CoV-2 [ ACS Infect Dis, 2020, acsinfecdis.0c00486] PubMed: 33183004
A high throughput screen for TMPRSS2 expression identifies FDA-approved and clinically advanced compounds that can limit SARS-CoV-2 entry [ Res Sq, 2020, rs.3.rs-48659] PubMed: 32818215
The Effect of Promiscuous Aggregation on in Vitro Drug Metabolism Assays [ Pharm Res, 2019, 36(12):170] PubMed: 31654151
Activation of the Anti-Aging and Cognition-Enhancing Gene Klotho by CRISPR-dCas9 Transcriptional Effector Complex [Chen CD, et al. J Mol Neurosci, 2018, 64(2):175-184] PubMed: 29352444
Quantitative High-Throughput Screening Using a Coincidence Reporter Biocircuit. [ Curr Protoc Neurosci, 2017, 79:5] PubMed: 28398644

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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