ML133 HCl

製品コードS2825 バッチS282501

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	C₁₉H₁₉NO.HCl
	分子量	313.82	CAS No.	1222781-70-5
Solubility (25°C)*	体外	DMSO	63 mg/mL (200.75 mM)
		Ethanol	6 mg/mL (19.11 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	ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.
in vitro	The ratio of total concentration of extracellular ML133 versus intracellular ML133 is 1:0.13 at pH 6.5, 1:9.09 at pH 8.5. ML133 is clean against 3A4 and 2C9 (IC50 >30 μM), displays moderate inhibition of 1A2 (IC50 = 3.3 μM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 μM) in CYP450 assay. ML133 is highly protein bound (>99%) in both human and rat and also displays high intrinsic clearance in both species. ML133 (10 μM) is not displaced by K⁺ influx from the wild-type K_ir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of K_ir2.1, especially D172 and I176. ^[1]

製品説明

ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.

in vitro

The ratio of total concentration of extracellular ML133 versus intracellular ML133 is 1:0.13 at pH 6.5, 1:9.09 at pH 8.5. ML133 is clean against 3A4 and 2C9 (IC50 >30 μM), displays moderate inhibition of 1A2 (IC50 = 3.3 μM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 μM) in CYP450 assay. ML133 is highly protein bound (>99%) in both human and rat and also displays high intrinsic clearance in both species. ML133 (10 μM) is not displaced by K⁺ influx from the wild-type K_ir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of K_ir2.1, especially D172 and I176. ^[1]

プロトコル(参考用のみ)

参考

[1] Wang HR, et al. ACS Chem Biol, 2011, 6(8), 845-856.

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：

Dextran sodium sulfate potentiates NLRP3 inflammasome activation by modulating the KCa3.1 potassium channel in a mouse model of colitis [ Cell Mol Immunol, 2022, 19(8):925-943]	PubMed: 35799057
Kir2.1-mediated membrane potential promotes nutrient acquisition and inflammation through regulation of nutrient transporters [ Nat Commun, 2022, 13(1):3544]	PubMed: 35729093
Memantine selectively prevented the induction of dynamic allodynia by blocking Kir2.1 channel and inhibiting the activation of microglia in spinal dorsal horn of mice in spared nerve injury model. [ Mol Pain, 2019, 15:1744806919838947]	PubMed: 30845882
Kir2. 1 Channel Regulation of Glycinergic Transmission Selectively Contributes to Dynamic Mechanical Allodynia in a Mouse Model of Spared Nerve Injury [Shi Y Neurosci Bull, 2018, 10.1007/s12264-018-0285-8]	PubMed: 30203408

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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