Amlodipine

製品コードS1905 バッチS190503

印刷

化学情報

Chemical Structure Synonyms UK-48340 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H25ClN2O5
分子量 408.88 CAS No. 88150-42-9
Solubility (25°C)* 体外 DMSO 82 mg/mL (200.54 mM)
Ethanol 82 mg/mL (200.54 mM)
Water 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.
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 6.000mg/ml (14.67mM) Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 6.000mg/ml (14.67mM) Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 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 Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
in vitro Amlodipine causes a dose-dependent increase in nitrite production. This compound also increases nitrite production in large coronary arteries and in aorta. [1] It is attributed to distinct membrane physico-chemical interactions. This chemical contributes to distinct membrane biophysical interactions that lead to potent lipid antioxidant effects, independent of calcium channel modulation. [2] It increases plaque smooth muscle cell content (P<0.05), whereas atenolol decreases plaque inflammation. [3] This compound attenuates intracellular neuronal Ca2+ increases elicited by KCl depolarization but does not affect Ca2+ changes triggered by N-methyl-D-aspartate receptor activation. It also inhibits free radical-induced damage to lipid constituents of the membrane in a dose-dependent manner, independent of Ca2+ channel modulation. [4]
in vivo Amlodipine results in regression of cardiovascular hypertrophy and amelioration of endothelial dysfunction in spontaneously hypertensive rats. [5] This compound significantly reduces aortic hypertrophy, endothelial dysfunction, LOX-1 expression, aortic O(2)(-) and ONOO(-) production, and plasma free 8-F(2)alpha-isoprostane levels in Ang II-infused rats. It has antihypertensive and antioxidant activity in vivo, which effectively inhibits many of the oxidative stress-dependent mechanisms involved in Ang II-mediated cardiovascular injury. [6]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/9494028/
  • https://pubmed.ncbi.nlm.nih.gov/10072734/
  • https://pubmed.ncbi.nlm.nih.gov/18391092/
  • https://pubmed.ncbi.nlm.nih.gov/10098848/
  • https://pubmed.ncbi.nlm.nih.gov/9797191/
  • https://pubmed.ncbi.nlm.nih.gov/14751660/

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：

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Targeting the core program of metastasis with a novel drug combination [ Cancer Med, 2024, 13(11):e7291] PubMed: 38826119
KCTD4 interacts with CLIC1 to disrupt calcium homeostasis and promote metastasis in esophageal cancer [ Acta Pharm Sin B, 2023, 13(10):4217-4233] PubMed: 37799381
KCTD4 interacts with CLIC1 to disrupt calcium homeostasis and promote metastasis in esophageal cancer [ Acta Pharm Sin B, 2023, 13(10):4217-4233] PubMed: 37799381
Anticancer Effects of Amlodipine Alone or in Combination With Gefitinib in Non-Small Cell Lung Cancer [ Front Pharmacol, 2022, 13:902305] PubMed: 35721193
Repurposing screen identifies Amlodipine as an inducer of PD-L1 degradation and antitumor immunity [ Oncogene, 2021, 40(6):1128-1146] PubMed: 33323966
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
Development and Feasibility of a Porcine Model of Amlodipine Toxicity. [ J Med Toxicol, 2020, 16(1):61-66] PubMed: 31385194
Induction of store-operated calcium entry (SOCE) suppresses glioblastoma growth by inhibiting the Hippo pathway transcriptional coactivators YAP/TAZ. [ Oncogene, 2019, 38(1):120-139] PubMed: 30082911
Selective uveal melanoma inhibition with calcium channel blockade. [ Int J Oncol, 2019, 55(5):1090-1096] PubMed: 31545410

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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