IndraLab

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MK-499 inhibits KCNH2. 6 / 6
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"The mean channel open times at -90 mV were 2.9 +/- 0.5 and 11.8 +/- 1.0 ms, and the mean channel closed times were 0.54 +/- 0.02 and 14.5 +/- 5.3 ms. Single HERG channels were blocked by MK-499, a class III antiarrhythmic agent that blocks I (Kr) in cardiac myocytes."
9087606
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"However, MK-499 did block HERG current if oocytes were repetitively pulsed, or clamped at a voltage positive to the threshold potential for channel activation."
8593709
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"Under steady state conditions, block of HERG by MK-499 was half maximal at 123 +/- 12 nmol/L at a test potential of -20 mV."
8593709
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"However, neither E-4031 nor MK-499 at a concentration of 1 IIM blocked HERG current, even after the incubation of the oocytes for up to 4 hr in these drugs."
7736582
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"1 For example, calcium activated IKCa1 channels are blocked by TRAM-34, 2 HERG1 is blocked by MK-499, 3 and voltage gated channels are blocked by bupivacaine."
17070844
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"Using the hERG1 D540K mutant that has the unusual property of opening in response to hyperpolarization, they confirmed that MK-499 blocked the hERG1 channel in the inner vestibule, as MK-499 was trapped by closure of the activation gate."
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