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Synonyms | CV-4093 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C35H38N4O6.2HCl |
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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 | |||
* <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. |
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. |
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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] |
細胞アッセイ | 細胞株 | Mesangial cells |
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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. |
Data from [Data independently produced by , , Antiviral Res, 2018, 150:130-136]
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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