Naftopidil

製品コードS2126 バッチS212601

印刷

化学情報

Chemical Structure Synonyms KT-611 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H28N2O3
分子量 392.49 CAS No. 57149-07-2
Solubility (25°C)* 体外 DMSO 17 mg/mL (43.31 mM)
Water Insoluble
Ethanol 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.

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生物活性

製品説明 Naftopidil (KT-611) は、α1-adrenergic receptor の選択的アンタゴニストであり、α1a、α1b、α1d に対する Ki 値はそれぞれ 3.7 nM、20 nM、1.2 nM です。これは、良性前立腺肥大症の治療に用いられます。
in vitro Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. This compound has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. It induces p21(cip1) but not p27(kip1) in PC-3 cells. This chemical induces apoptosis in all the investigated malignant mesothelioma cells, and a similar effect is obtained with prazosin, another α1-adrenoceptor blocker. Its-induced reduction in cell viability is inhibited by GF109203X, while prazosin-induced in cell viability is less affected. This compound, an alpha 1-adrenoreceptor antagonist produces a concentration-dependent inhibition ofcollagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 mM of it. It also inhibits the adrenaline-induced rise in [Ca2+]i in a concentration-dependent manner (30 mM doxazosin), significant inhibitions of platelet aggregation also being produced. This chemical (0.3, 1, and 3 μM) inhibits 5-HT-induced bladder contraction in a concentration-dependent manner. It inhibits both the 5-HT(2A) and 5-HT(2) receptor agonists-induced bladder contractions. This compound binds to the human 5-HT(2A) and 5-HT(2B) receptors with pKi values of 6.55 and 7.82, respectively.
in vivo Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. This compound inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/10361884/
  • https://pubmed.ncbi.nlm.nih.gov/17918159/
  • https://pubmed.ncbi.nlm.nih.gov/23482758/
  • https://pubmed.ncbi.nlm.nih.gov/9146854/
  • https://pubmed.ncbi.nlm.nih.gov/23274492/

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：

Changes in adrenoceptor expression level contribute to the cellular plasticity of glioblastoma cells [ J Physiol Sci, 2025, 75(2):100016] PubMed: 40184918
Quantifying Drug Combination Synergy along Potency and Efficacy Axes. [ Cell Syst, 2019, 8(2):97-108] PubMed: 30797775

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。