KB-130015 - CAS:147030-48-6

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KB-130015 (Synonyms:2,6-二碘-4-[(2-甲基苯并呋喃-3-基)甲基]-苯氧基乙酸;2-[2,6-二碘-4-[(2-甲基-3-苯并呋喃基)甲基]苯氧基]乙酸)

目录号 : KCM11506 CAS No. : 147030-48-6 纯度 : ≥95%

Data Sheet SDS 产品使用指南

KB-130015 is an antiarrhythmic agent and a derivative of amiodarone . It inhibits potassium currents induced by acetylcholine or adenosine in isolated guinea pig atrial myocytes (ICs = 0.82 and 0.57 µM, respectively). KB-130015 activates or inhibits the voltage-gated potassium channel human-ether-a-go-go (hERG), also known as K11.1, in HEK293 cells in a voltage-dependent manner. It activates large-conductance calcium-activated potassium (K1.1/BK) channels in HEK293 cells expressing the K1.1 subunit Slo1 (EC = 20.2 μM). KB-130015 (40 mg/kg) prolongs the duration of electrically stimulated action potentials in guinea pig papillary muscle ex vivo. It is also an antagonist of human thyroid hormone receptor α (TRα) and TRβ (ICs = 2.2 and 4.1 µM, respectively, in reporter assays).

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1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

KB130015 is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC₅₀ values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 activates hERG1 channels (EC₅₀ = 12.2 μM) and large-conductance Ca²⁺-activated K⁺ (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease.

体外研究

KB130015 (1-10 μM) slows down the inactivation kinetics of cardiac Na⁺channels in guinea pig, rabbit, and rat ventricular myocytes by enhancing slow inactivation I_Na components and reducing fast inactivation components [2].

KB130015 shifts the steady-state voltage dependent inactivation of Na⁺channels towards a more negative potential and slows down the recovery of cardiac muscle cells after inactivation [2].

KB130015 (10 μM) reduced the amplitude of L-type Ca²⁺current (Ica-L) by about 30% in rat ventricular myocytes, but did not alter its inactivation time course [2].

KB130015 (50 μM) exerts positive inotropic effects by increasing the cell shortening amplitude of rat ventricular myocytes without altering the time course [2].

KB130015 (100 μM) shortened action potential duration (APD) in rat ventricular trabeculae, but prolonged short APD and induced early depolarization (EADs) in mouse left ventricular papillary muscles [2].

KB130015 (100 μM) activates large conductance Ca²⁺- activated K⁺(BKCa) channels composed of hSlo1 (α) subunits in HEK 293 cells, as well as insect (fruit fly dSlo and American cockroach pSlo) BKCa channels expressed in HEK 293 cells.

体内研究

KB130015 (40 mg/kg, intraperitoneal injection, once daily, 20 days) significantly prolonged APD50, APD90, and ERP in guinea pig ventricular papillary muscles, reduced Vmax, and did not alter APA and RP [1].
KB130015 (30-300 mg/kg, orally, once daily, 2 weeks) altered thyroid hormone levels (decreased T3, increased T4 and TSH) in Sprague Dawley rats [1].
KB130015 (20 mg/kg, intraperitoneal injection, once daily, 20 days) inhibits ventricular premature beats, ventricular tachycardia, and ventricular fibrillation during ischemia and reperfusion in rabbits with left anterior descending artery occlusion.

Animal Model:	Sprague-Dawley rats (each group consisting of 5 males and 5 females)
Dosage:	30, 100, 300 mg/kg
Administration:	p.o. daily for 2 weeks
Result:	Reduced serum T3 and increased serum T4 and TSH. Increased serum cholesterol only in males at 300 mg/kg. Caused mild increases in ASAT and ALAT at 300 mg/kg. Had no effect on weight gain.

Animal Model:	Rabbits with ischemia and reperfusion were established by 30-min occlusion of the left anterior descending artery
Dosage:	20 mg/kg
Administration:	i.p. daily for 20 days
Result:	Increased TSH and T4 plasma levels in chronically treated rabbits. Remained active during treatment with no difference in weight gain compared to vehicle-treated rabbits. Suppressed ventricular premature beats, ventricular tachycardia and fibrillation associated with ischemia and reperfusion periods in rabbits with left anterior descending artery occlusion.

分子式

C₁₈H₁₄I₂O₄

分子量

548.1103

CAS号

147030-48-6

中文名称

2,6-二碘-4-[(2-甲基苯并呋喃-3-基)甲基]-苯氧基乙酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (182.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8245 mL	9.1223 mL	18.2445 mL
5 mM	0.3649 mL	1.8245 mL	3.6489 mL
10 mM	0.1824 mL	0.9122 mL	1.8245 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂：10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂：10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥95%

Data Sheet

SDS

产品使用指南

[1]. Carlsson B, et al. Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J Med Chem. 2002 Jan 31;45(3):623-30.

[2]. Mubagwa K, Macianskiene R, Viappiani S, Gendviliene V, Carlsson B, Brandts B. KB130015, a new amiodarone derivative with multiple effects on cardiac ion channels. Cardiovasc Drug Rev. 2003 Fall;21(3):216-35.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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体积

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动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器