Felodipine

製品コードS1885 バッチS188503

印刷

化学情報

Synonyms

CGH-869

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₉Cl₂NO₄

分子量

384.25

CAS No.

72509-76-3

Solubility (25°C)*

体外

DMSO

77 mg/mL (200.39 mM)

Ethanol

72 mg/mL (187.37 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 1 40%PEG300 2 5%Tween80 3 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。	3.850mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 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.
Clear solution	5% DMSO 1 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。	1.900mg/ml (4.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 38 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.

* <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	Felodipine (CGH-869) is a selective L-type Ca²⁺ channel blocker with IC50 of 0.15 nM.
in vitro	Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca²⁺ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM). ^[1] This compound significantly induces the transcription and secretion of IL-6 and IL-8 with ED50 values of 5.8 nM and 5.3 nM in primary human VSMC and lung fibroblasts, respectively, while propranolol or furosemide fails to affect the expression of the two IL genes. ^[2] It blocks the muscarinic receptor-mediated (carbachol) Ca²⁺-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM. ^[3] This chemical at low concentration of 0.1 μM is sufficient to increases NOx generation, Ca²⁺-dependent NOS activity, and eNOS protein mass in rat endothelial cells. ^[4] It (10 μM) reduces nuclear translocation of p42/44 mitogen-activated protein kinase and Elk-1 activation stimulated by PDGF-BB, leading to the inhibition of human SMC proliferation. ^[5] It modestly blocks the Ca_v3.2 T-type Ca²⁺-channel with an IC50 of 6.8 μM. ^[6]
in vivo	Oral administration of Felodipine significantly reduces the average blood pressure (BP) in rats with 5/6 renal ablation, but causes additional impairment of the already impaired renal autoregulation. ^[7] Administration of this compound significantly reduces systolic blood pressure (SBP), serum insulin, intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by blocking NF-κB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response. ^[8]
特徴	Unlike many Ca²⁺ channel blockers, Felodipine does not have cardiac side effects due to high selectivity for vascular smooth muscle vs. myocardial tissue.

プロトコル(参考用のみ)

キナーゼアッセイ	The effect of Felodipine on tension in coronary segments
キナーゼアッセイ	The cylindrical coronary segments from porcine hearts are inverted and fixed horizontally between a stationary bottom pin and a top pin connected to the lever of a force-displacement transducer precalibrated with standard weights on a Grass model 5D polygraph. The cylindrical segments are bathed in 25 mL of PSS in a water jacketed tissue bath at 37 °C. The bath solution is bubbled continuously with a mixture of 95% O₂-5% CO₂. An initial resting tension of 10 g is set during a 2-hour equilibration period. After the equilibration, three to four successive contraction-relaxation cycles are induced with 35 mM KCl and subsequent washes with PSS until reproducible contractions are obtained. After the final response reached and maintained steady tension (16-25 g above resting tension), a cumulative dose-response curve for Felodipine is obtained. Additional aliquots of this compound are added only after the response to the previous dose has plateaued. The concentration of this chemical that half-maximally relaxes the coronary from KCl-induced contraction (IC50) is determined from dose response curv
動物実験	動物モデル	Male Sprague-Dawley rats with approximately 5/6 renal ablation
	投薬量	1 g/kg/day
	投与方法	Orally

参考

https://pubmed.ncbi.nlm.nih.gov/6875846/
https://pubmed.ncbi.nlm.nih.gov/8576944/
https://pubmed.ncbi.nlm.nih.gov/8917646/

https://pubmed.ncbi.nlm.nih.gov/9774369/
https://pubmed.ncbi.nlm.nih.gov/11744032/
https://pubmed.ncbi.nlm.nih.gov/18974361/

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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
Felodipine enhances aminoglycosides efficacy against implant infections caused by methicillin-resistant Staphylococcus aureus, persisters and biofilms [ Bioact Mater, 2022, 14:272-289]	PubMed: 35310349
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
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

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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