Manidipine 2HCl

製品コードS2482 バッチS248203

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 100 mg/mL (146.28 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）
Clear solution
2%DMSO 30%PEG300 68%ddH2O
2.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 100 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 680 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 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. [1] 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. [2] 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. [3] In addition, Manidipine, at nanomolar concentrations, is efficacious in modulating gene transcriptions that are involved in proinflammatory changes of mesangial cells. [4]
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. [5] When Manidipine is administered at 10 μg/kg, the hypotensive action is markedly augmented. [6] 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. [7]

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.

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：

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。