1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. MK-8153

MK-8153 是一种有效的,选择性和具有口服活性的肾外髓质钾通道 (ROMK) 抑制剂,对 ROMK EP 和 hERG EP 的 IC50 值分别为 5 nM 和 34 μM。MK-8153 可用作利尿剂。

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MK-8153 Chemical Structure

MK-8153 Chemical Structure

CAS No. : 1548286-45-8

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1 mg ¥4300
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5 mg ¥9450
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-8153 is a potent, selective and orally active inhibitor of renal outer medullary potassium channel (ROMK), with IC50s of 5 nM, 34 μM for ROMK electrophysiology (EP) and hERG EP, respectively. MK-8153 can be used as the diuretic/atriuretic[1].

IC50 & Target

IC50: 5 nM (ROMK EP), 34 μM (hERG EP)[1]

体外研究
(In Vitro)

MK-8153 inhibits current through rat ROMK, rKir1.1/HEK293 cells in electrophysiological recordings with an IC50 of 2.5 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MK-8153 (0.1-10 mg/kg/d, p.o. once daily for 3 days) causes a dose-dependent decrease in systolic blood pressure of aged SHRs. MK-8153 shows diuretic effects in SHRs[1].
MK-8153 (2 mg/kg; p.o.) exhibits terminal elimination half-lives (rat 3.6, dog 9.1, Rhesus 3.3 h), bioavailability (rat 53%, dog ~100%, Rhesus 3.4%), and plasma clearance (rat 29.4, dog 8.7, Rhesus 58.3 mL/min/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Aged spontaneously hypertensive rats (SHRs)[1]
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: P.o. once daily for 3 days
Result: Observed the maximal lowering of systolic blood pressure (∼24 mm Hg) by day 3 at the 3 mg/kg.
Dose-dependently increased the sodium excretion.
分子量

440.49

Formula

C24H28N2O6

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MK-8153
目录号:
HY-132201
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