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ML133 HCl

ML133 HCl

Item no.	S2825-10
Manufacturer	Selleckchem
CASRN	1222781-70-5
Amount	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 25 mg 5 mg 50 mg 5 g
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Smiles	COC1=CC=C(C=C1)CNCC2=CC=CC3=CC=CC=C32.Cl
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	Kir2.1,Potassium Channel
Similar products	ML133
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	313, 82
IC50	290 nM [1], 290 nM [1], 290 nM [1], 290 nM [1], 290 nM [1], 290 nM [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 uM), displays moderate inhibition of 1A2 (IC50 = 3.3 uM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 uM) 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 uM) is not displaced by K+ influx from the wild-type Kir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of Kir2.1, especially D172 and I176. [1]
Solubility (25C)	DMSO 63 mg/mL, Water <1 mg/mL, Ethanol 6 mg/mL
Information	ML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.
Chemical Name	1-Naphthalenemethanamine, N-[(4-methoxyphenyl)methyl]-, hydrochloride (1:1)

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S2825-10-datasheet.pdf

S2825-10-safety-datasheet.pdf