ML133 HCl 1222781-70-5

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Molecular Weight:

313.82 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.

Biological Activity

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 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

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Product Categories : Transmembrane Transporters > Potassium Channel Inhibitor