R-IMPP

製品コードS8420 バッチS842001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₇N₃O₂
	分子量	389.49	CAS No.	2133832-83-2
Solubility (25°C)*	体外	DMSO	77 mg/mL (197.69 mM)
		Ethanol	77 mg/mL (197.69 mM)
		Water	7 mg/mL (17.97 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	R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.
in vitro	R-IMPP promotes uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but instead causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is discovered that exhibited weak PCSK9 anti-secretagogue activity (half maximal inhibitory concentration [IC50] = 4.8 μM), but does not affect intracellular ATP levels in the recombinant CHO-K1 cells, a measure of cytotoxicity, nor decrease secretion of a control protein, secreted alkaline phosphatase, a measure of relative selectivity. The inhibitory response of R-IMPP is stereospecific^[1].

製品説明

R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.

in vitro

R-IMPP promotes uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but instead causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is discovered that exhibited weak PCSK9 anti-secretagogue activity (half maximal inhibitory concentration [IC50] = 4.8 μM), but does not affect intracellular ATP levels in the recombinant CHO-K1 cells, a measure of cytotoxicity, nor decrease secretion of a control protein, secreted alkaline phosphatase, a measure of relative selectivity. The inhibitory response of R-IMPP is stereospecific^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Huh7 cells
	濃度	10, 30 μM
	反応時間	24 h
	実験の流れ	Huh7 cells are plated at 150,000 cells per well and transfected with the full-length and truncation mutants. After 24 hr, cells are treated with vehicle, 30 μMR-IMPP, or 30 μM S-IMPP. At 48 hr post-transfection, cells are washed three times with TBS +2 mg/mL BSA and lysed with 100 mL of RIPA buffer per well. Protein lysates are subjected to SDS-PAGE and western blot analysis for PCSK9 (V5) and b-actin.

参考

[1] Petersen DN, et al. Cell Chem Biol. 2016, 23(11):1362-1371.

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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