Lacidipine

製品コードS1994 バッチS199401

印刷

化学情報

Chemical Structure Synonyms GX-1048, GR-43659X, SN-305 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H33NO6
分子量 455.54 CAS No. 103890-78-4
Solubility (25°C)* 体外 DMSO 91 mg/mL (199.76 mM)
Ethanol 22 mg/mL (48.29 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.
* <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 Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
in vitro Lacidipine, an L-type Ca(2+) channel blocker that also inhibits [Ca(2+)](ER) efflux, enhances folding, trafficking, and activity of degradation-prone glucocerebrosidase (GC) variants. This compound remodels mutated GC proteostasis by simultaneously activating a series of distinct molecular mechanisms, namely modulation of Ca(2+) homeostasis, upregulation of the ER chaperone BiP, and moderate induction of the unfolded protein response. [1] It almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages. [2]
in vivo Lacidipine has non-significant effects on blood pressure but inhibits the paradoxical increases in plasma renin activity (PRA) and in renin mRNA in kidney that are found in salt-loaded stroke-prone spontaneously hypertensive rats (SHRSP). This compound restores the physiological downregulation of renin production by high salt and reduces left ventricular hypertrophy and mRNA levels of atrial natriuretic factor and transforming growth factor-beta1. [3] This chemical (1 and 3 mg/kg) also effectively increases calcium concentrations significantly in ovariectomized rats. [4] This dihydropyridine-type calcium antagonist reduces the cardiac hypertrophy and the cardiacendothelin-1 (ET-1) gene overexpression occurring in salt-loaded stroke-prone spontaneously hypertensive rats (SL-SHRSP), an effect occurring without systolic blood pressure (SBP) change. It exerts a dose-related inhibition of ventricle hypertrophy and preproET-1-mRNA expression in SHRSP and indicate that this effect is unrelated to SBP changes. [5]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/21700212/
  • https://pubmed.ncbi.nlm.nih.gov/9401788/
  • https://pubmed.ncbi.nlm.nih.gov/11724758/
  • https://pubmed.ncbi.nlm.nih.gov/17936271/
  • https://pubmed.ncbi.nlm.nih.gov/8762091/

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
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704

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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