Manidipine 2HCl

製品コードS2482 バッチS248202

印刷

化学情報

Chemical Structure Synonyms CV-4093 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C35H38N4O6.2HCl
分子量 683.62 CAS No. 89226-75-5
Solubility (25°C)* 体外 DMSO 137 mg/mL (200.4 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 Manidipine 2HCl (CV-4093) は、IC50が2.6 nMのcalcium channelブロッカーであるManidipineのHCl塩形態であり、降圧剤として臨床的に使用されています。フェーズ4。
in vitro At a holding potential of −37 mV, Manidipine decreases the Ca2+ current at concentrations above 0.1 nM, and abolishes it at 100 nM. Manidipine concentration-dependently inhibits the calcium concentration response curves. Manidipine inhibits coronay artery and renal artery with pIC50 of 9.3 nM and 9.1 nM, respectively. Manidipine partly inhibits sympathetic nerve activity and suppresses the mean arterial pressure response to infused norepinephrine. Manidipine also inhibits aldosterone secretion. Manidipine increases in both urinary calcium and uric acid. In addition, Manidipine, at nanomolar concentrations, is efficacious in modulating gene transcriptions that are involved in proinflammatory changes of mesangial cells.
in vivo Manidipine (3 mg/kg and 10 mg/kg, p.o.) dose-dependently decreases systolic blood pressure in the three types of hypertensive rats. At the dose of 10 mg/kg, Manidipine decreases the blood pressure to the normotensive level between 1 hour and 3 hours after Manidipine is administered; the antihypertensive effect lasted for at least 8 hours. When Manidipine is administered at 10 μg/kg, the hypotensive action is markedly augmented. Manidipine potently inhibits the Ca inward current, When the potential is at -60 mV. Manidipine consistently inhibits the Ca current evoked by depolarization to 0 mV. However, a low concentration of Manidipine (1-3 nM) enhances the Ca current evoked by the depolarizing pulse of -20 mV, when the membrane potential is held at -80 mV. Inhibition of the Ca current induced by Manidipine develops slowly and over 10 minutes is required to reach the maximum inhibition.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mesangial cells
濃度 10 nM
反応時間 Days 1, 3 and 5
実験の流れ The mitogenic effect is measured by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, 1 × 105 quiescent cells is seeded into a 25-mL cell culture bottle and kept in low serum medium (0.1% FCS). On the following day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. The medium is replaced each day, and the cells are counted at days 1, 3 and 5.
動物実験 動物モデル Normotensive male Wistar-Kyoto rats and male stroke-prone SHR
投薬量 1 mg/kg, 3 mg/kg and 10 mg/kg
投与方法 Administered via p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/8287905/
  • https://pubmed.ncbi.nlm.nih.gov/8430602/
  • https://pubmed.ncbi.nlm.nih.gov/8430610/
  • https://pubmed.ncbi.nlm.nih.gov/1570335/
  • https://pubmed.ncbi.nlm.nih.gov/3210447/
  • https://pubmed.ncbi.nlm.nih.gov/2593383/
  • https://pubmed.ncbi.nlm.nih.gov/3681701/

カスタマーフィードバック

Data from [Data independently produced by , , Antiviral Res, 2018, 150:130-136]

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：

UGT8 mediated sulfatide synthesis modulates BAX localization and dictates apoptosis sensitivity of colorectal cancer [ Cell Death Differ, 2024, 10.1038/s41418-024-01418-y] PubMed: 39580596
Selective Translation of Maternal mRNA by eIF4E1B Controls Oocyte to Embryo Transition [ Adv Sci (Weinh), 2023, 10(11):e2205500] PubMed: 36755190
HCMV-IE2 promotes atherosclerosis by inhibiting vascular smooth muscle cells' pyroptosis [ Front Microbiol, 2023, 14:1177391] PubMed: 37234524
Evidence for Specific Receptor-Mediated Toxicity of Pharmaceuticals in Aquatic Organisms Derived from Acute and Chronic Standard Endpoints [ Environ Toxicol Chem, 2021, 10.1002/etc.5018] PubMed: 33595135

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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