Netupitant

製品コードS4654 バッチS465401

印刷

化学情報

Chemical Structure Synonyms CID6451149, CID 6451149, CID-6451149 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C30H32F6N4O
分子量 578.59 CAS No. 290297-26-6
Solubility (25°C)* 体外 Ethanol 100 mg/mL (172.83 mM)
DMSO 2 mg/mL (3.45 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 Netupitant (CID6451149) is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity.
in vitro In CHO NK1 cells, Netupitant concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB 8.87). In cells expressing NK2 or NK3 receptors, Netupitant is inactive[1].
in vivo Netupitant behaves as a brain penetrant, orally active, potent and selective NK1 antagonist. In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that is dose-dependently inhibited by Netupitant given intraperitoneally in the 1-10 mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID50 1.5 mg/kg) or orally (ID50 0.5 mg/kg). In time course experiments in gerbils Netupitant displayed long lasting effects[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NG108-15 cells
濃度 1, 3, 10, 30 nM
反応時間 1 h
実験の流れ

cells are preincubated for 1 h at 37℃ with either growth media alone(control) or media containing antagonists. Antagonist concentrations are at least 30-fold the Kd value to ensure receptor saturation. After preincubation, antagonists are removed and cells are rinsed with growth media alone for an additional hour to allow for dissociation of antagonists still bound to receptor.Cell media are then replaced with isosmotic HEPES buffer (pH 7.4, 20 mM) containing NaCl (130 mM), KCl (2 mM), MgCl2 (1 mM) CaCl2 (2 mM), Fluo-4 acetoxymethyl (AM) ester (2 mM), pluronic acid (0.04%) and SP at various concentrations in the 3 nM to 1 mM range. The final incubation lasted for 1 h at 37 ℃. Pluronic acid is added as a nonionic surfactant to sequester the AM ester molecules into micelles for cellular uptake.
動物実験 動物モデル Male Swiss mice
投薬量 1 and 10 mg/kg
投与方法 i.p.

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：

Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists. [ Nat Commun, 2019, 10(1):17] PubMed: 30604743

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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