Encequidar (HM30181)

製品コードS3431 バッチS343101

化学情報

	Synonyms	HM30181A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₈H₃₆N₆O₇
	分子量	688.73	CAS No.	849675-66-7
Solubility (25°C)*	体外	DMF	50 mg/mL warmed with 50ºC water bath (72.59 mM)
		DMSO	Insoluble
		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	Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).
in vitro	HM30181 potently and selectively inhibits Pgp-mediated efflux transport of rhodamine 123 in CCRF-CEM T cells with 13.1±2.3 nM.^[1]
in vivo	PET scans with the Pgp substrate (R)-[¹¹C]verapamil in FVB wild-type mice pretreated i.v. with HM30181 (10 or 21 mg/kg) fails to show significant increases in (R)-[¹¹C]verapamil brain uptake compared with vehicle treated animals.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CCRF-CEM T lymphoblast cells
	濃度	1-100 nM
	反応時間	5 min
	実験の流れ	Briefly, cells expressing wild-type Pgp (CCRF-CEM T lymphoblast cell line) were sedimented, the supernatant was removed by aspiration, and the cells were resuspended in Dulbecco’s Modified Eagle’s Medium (DMEM) containing rhodamine 123 at a final concentration of 0.2 μg/ml (0.53 μM). Cells were loaded with fluorochrome for 30 min at 37°C. Tubes were chilled on ice and cells were harvested at 500 × g in an Eppendorf 5403 centrifuge. The cell pellet was washed with ice cold DMEM medium (pH 7.4) and again centrifuged at 500 × g. After resuspension, aliquots of the cell suspension, each containing approximately 1 × 10<sup>6</sup> were transferred to individual fluorescence-activated cell sorter (FACS) tubes and again centrifuged. Supernatants were removed, and the pellets were resuspended individually in prewarmed DMEM medium (pH 7.4) containing either no inhibitor or HM30181 mesylate or elacridar hydrochloride or tariquidar dimesylate at various concentrations in DMSO ranging from 1 to 100 nM. Right after resuspending cells each individual tube was placed in a temperature controlled unit and cell associated fluorescence was monitored over a period of 5 min with a FACS system.
動物実験	動物モデル	Female Mdr1a/b(−/−), Bcrp1(−/−) and Mdr1a/b(−/−)Bcrp1(−/−) mice with a FVB genetic background
	投薬量	10 or 21 mg/kg
	投与方法	i.v.

参考

[1] Florian Bauer, et al. Eur J Pharmacol. 2012 Dec 5;696(1-3):18-27.

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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