APD668

製品コードS6746 バッチS674601

印刷

化学情報

Chemical Structure Synonyms JNJ28630368 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C21H24FN5O5S
分子量 477.51 CAS No. 832714-46-2
Solubility (25°C)* 体外 DMSO 96 mg/mL (201.04 mM)
Ethanol 2 mg/mL (4.18 mM)
Water 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 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
in vitro

APD668 is shown to increase adenylate cyclase activation in HEK293 cells transfected with human GPR119 (but not in non-transfected cells) in a concentration-dependent manner with an EC50 of 23 nM. APD668 also enhanced insulin release from both rat and human isolated pancreatic islets in a glucose-dependent manner. In a standard panel of around 80 known receptors and ion channels, APD668 did not show any binding in excess of 50% of control to any other proteins at concentrations up to 10 μM[1].
in vivo

Chronic treatment with APD668 showed that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 is highly bound to plasma proteins of male and female cynomolgus monkeys and humans (P99%), but was less extensively bound to male (93.0%) and female (96.6%) rats. In pharmacokinetic assessments across multiple species using single oral doses of APD668, absorption was rapid to moderate (Tmax 62 h) in mice, Sprague-Dawley (SD) rats, and monkeys, but slower in dogs (Tmax = 6 h) and showed a dose-dependent increase in rats and monkeys. In general, exposure was dose-dependent at lower doses and appeared to plateau at doses greater than 300 mg/kg. Exposure was greater in female rats compared with males. Absolute oral bioavailability was moderate to good in mice, rats, and monkeys (44–79%), but was lower in dogs (22%). The volume of distribution (Vdss) values were somewhat variable ranging from 0.1 L/kg in monkey to 2.6 L/kg in rats. Elimination, based on mean T1/2 after intravenous (iv) dosing, was rapid to moderate in mice, rats, dogs, and monkeys (0.8-3.9 h). The pharmacokinetic profile of APD668 in Zucker fa/fa rats was somewhat different from that in SD rats. After oral administration, the tmax and T1/2 were longer, and the AUC and the oral bioavailability were greater in the Zucker compared with the SD rats. Following iv administration, the Zucker rats also had larger AUC values, longer T1/2 values and greater Vdss values[1].

プロトコル(参考用のみ)

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。