BMY 7378 Dihydrochloride

製品コードS2691 バッチS269101

印刷

化学情報

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

C22H31N3O3.2HCl
分子量 458.42 CAS No. 21102-95-4
Solubility (25°C)* 体外 DMSO 92 mg/mL (200.68 mM)
Water 92 mg/mL (200.68 mM)
Ethanol 20 mg/mL (43.62 mM)
体内 （毎回新しく調製した物を用意してください）
Clear solution
Saline
15.0mg/ml Taking the 1 mL working solution as an example, add 15 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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 BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.
in vitro BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54. [1] BMY 7378 is selective for the α1D-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; rat α1d-adrenoceptor 8.2, human α1d-adrenoceptor 9.4 [2] BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. [3]
in vivo BMY 7378 (pA2 of 8.67) is approximately 100 times more potent than yohimbine (pA2 of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA2 of 6.48) is approximately 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-adrenoceptor).[1] BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Radioligand Binding Assays
Rat kidney membranes and membranes of Sf9 cells expressing human recombinant α2C -adrenoceptors are prepared. The resultant pellets are used immediately or stored at -20 °C for later use.Pellets are reconstituted in 10 volumes (kidney) or 25 volumes (Sf9 cells) of incubation buffer. In saturation experiments, aliquots of membrane suspension are incubated with various concentrations of [3H]-yohimbine (specific activity: 81 Ci mmol-1) at 25 °C (rat kidney: 0.5-30 nM; Sf9 cells: 0.2-20 nM; rat submandibular gland: 1.0-40 nM; incubation buffer: Tris-HCl 50 mM, EDTA 5 mM, pH 7.4 at 25 °C). In competition studies, [3H]-yohimbine (5 or 10 nM) is incubated with competing ligands in concentrations from 0.1 nM to 1 mM in 0.5 log unit increments for 30 min. Non-specific binding is determined in the presence of phentolamine (10 lM). Specific binding of [3H]-yohimbine is 70-90% of total binding at the concentration used in displacement experiments. Assays are terminated by washing with ice-cold incubation buffer, followed by rapid vacuum filtration through Whatman GF/C filters, using a Brandel Cell Harvester. Radioactivity retained on filters is determined by liquid scintillation spectroscopy.
動物実験 動物モデル rats
投薬量 0.25-5 mg/kg
投与方法 Inject subcutaneously at a single dose

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。