Ciproxifan Maleate

製品コードS2813 バッチS281301

印刷

化学情報

Chemical Structure Synonyms FUB 359 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H18N2O2.C4H4O4
分子量 386.4 CAS No. 184025-19-2
Solubility (25°C)* 体外 DMSO 54 mg/mL (139.75 mM)
Ethanol 54 mg/mL (139.75 mM)
Water 1 mg/mL (2.58 mM)
* <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 Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.
in vitro Ciproxifan inhibits [3H]HA release from synaptosomes with Ki of 0.5 nM. Ciproxifan inhibits the binding of [125I]iodoproxyfan at the brain H3 receptor with Ki of 0.7 nM. Ciproxifan displays high affinity at H3 receptor but shows low apparent affinity at other receptor subtypes as evaluated in functional tests on isolated organs (histamine H1 and H2, muscarinic M3, adrenergic α1D and β1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4). [1]
in vivo Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. [1] Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. [3] Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. [4] Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Histamine H3 receptor assay
Longitudinal muscle strips from guinea pig small intestine are dissected out and incubated in a gassed O2/CO2 (95%/5%) modified Krebs-Ringer's bicarbonate medium at 37 °C in presence of 1 μM mepyramine to block the H1 receptor. After equilibration, contractile activity under stimulation (rectangular pulses of 15 V, 0.5 msec, 0.1 Hz) is recorded. Concentration-response curves of the effect of (R)α-MeHA alone or together with Ciproxifan are established.
動物実験 動物モデル Male Swiss mice
投薬量 1 mg/kg
投与方法 Intravenous or oral adminstration

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：

Inhibition of histamine receptor H3 suppresses the growth and metastasis of human non-small cell lung cancer cells via inhibiting PI3K/Akt/mTOR and MEK/ERK signaling pathways and blocking EMT [ Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00548-6] PubMed: 33159174
Inhibition of histamine receptor H3R suppresses prostate cancer growth, invasion and increases apoptosis via the AR pathway [Chen J, et al. Oncol Lett, 2018, 16(4):4921-4928] PubMed: 30250558

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。