Vericiguat

製品コードS9693 バッチS969301

印刷

化学情報

Chemical Structure Synonyms BAY1021189 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C19H16F2N8O2
分子量 426.38 CAS No. 1350653-20-1
Solubility (25°C)* 体外 DMSO 85 mg/mL (199.35 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Vericiguat (BAY1021189) is a potent, orally available and soluble guanylate cyclase (sGC) stimulator.
in vitro

The stimulation of sGC by Vericiguat is examined with a recombinant CHO cell line overexpressing rat sGC. Vericiguat stimulates the sGC reporter cell line concentration dependently with an EC50 of 1005 ± 145 nM. In the presence of the NO donor S-nitroso-N-acetyl-D,L-penicillamine (SNAP) (30 and 100 nM), the EC50 value shifts to 39.0 ± 5.1 and 10.6 ± 1.7 nM, respectively. In the presence of ODQ, pretreatment of the sGC reporter cell line with 10 μM ODQ for 3 h results in a significantly reduced efficacy of Vericiguat, with an EC50 of 256 ± 40 nM being observed.[1]
in vivo

Vericiguat can maintain heart and kidney function in a model of hypertension-induced end-organ damage with substantially reduced overall mortality.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 CHO cells
濃度 0.01 μM to 100 μM
反応時間 6 min
実験の流れ

Cells are plated in a volume of 25 μL on white 384-well Greiner Bio-One microplates and are cultured for 1 or 2 d in medium. Medium is removed, and cells are loaded for 3 h with calcium-free Tyrode-containing coelenterazine. Serial dilutions of the test compounds (including Vericiguat) in a volume of 10 μL in calcium-free Tyrode are applied to the cells for 6 min. Thereafter, 35 μL of Tyrode-containing calcium (final concentration: 3 mM) is added to the cells and the emitted light is measured for 40 s using a CCD camera in a light-tight box. The minimal effective concentration (MEC) is determined as the concentration where a ≥3-fold increase in the basal luminescence value is observed.
動物実験 動物モデル renin transgenic rats (RenTG)
投薬量 3 mg/kg, 10 mg/kg
投与方法 Oral gavage

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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