Compound 11

製品コードE0363 バッチE036301

化学情報

	Synonyms		Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₀H₁₂N₄O₂
	分子量	220.23	CAS No.	842964-18-5
Solubility (25°C)*	体外	DMSO	44 mg/mL (199.79 mM)
		Ethanol	4 mg/mL (18.16 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	Compound 11, a non-toxic and selective δ-secretase inhibitor (IC50=0.7 μM, in fluorescence-based assay) that interacts with both the active site and allosteric site of δ-secretase in Co-crystal structure analysis. The IC50 value of the compound 11 towards δ-secretase in Pala cells is 0.8 μM.
in vitro	Compound 11 inhibit δ-secretase in Pala cells, with an IC⁵⁰ of 7 μM. Compounds 11 is highly permeable assessed by Caco-2 monolayer permeability screen. The human liver microsomal stability screen demonstrates that following 30 min of incubation, 76% of compound 11 remained in human liver microsomes.^[1]
in vivo	Chronic treatment with δ-secretase inhibitor 11 markedly decreases the brain asparaginyl endopeptidase (AEP) activity, reduces the generation of Aβ1-40/42 and ameliorates memory loss. The inhibition of AEP with this reagent not only reduces the AEP-cleaved tau fragments and tau hyperphosphorylation, but also attenuates neuroinflammation in the form of microglial activation. Treatment with δ-secretase inhibitor 11 prevents the synaptic loss and alleviated dendritic disruption in senescence-accelerated mouse prone 8 (SAMP8) mouse brain.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Pala cells, HepG2 cells
	濃度	24 h
	反応時間	50 μM
	実験の流れ	Cells are incubated with various concentrations of compound 11 with the Pala cells for 2 h at 37 °C. Cells are collected, washed twice with PBS and lysed in Lysis Buffer. The protein concentrations are normalized via a Bradford assay and lysates are assayed with 5 μM Cbz-Ala-Ala-Asn-AMC.
動物実験	動物モデル	senescence-accelerated mouse prone 8 (SAMP8) mice
	投薬量	10 mg/kg
	投与方法	o.g.

参考

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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