KB130015
Based on 1 publication(s) in Google Scholar
KB130015 (KB015) 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.
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- Purity: 98.45%
- CAS No.: 147030-48-6
- 화학식: C18H14I2O4
- 분자량:548.11
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) KB130015
MoreAll Calcium Channel Isoforms
More
Biological Activity
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ThRα 4.5 μM (IC50) |
ThRβ 5.1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
>10 μM
Compound: 7 (KB130015)
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Agonism of compound towards thyroid response element (TRAF alpha) in CHO-K1 cells
Agonism of compound towards thyroid response element (TRAF alpha) in CHO-K1 cells
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[PMID: 11806713] |
| CHO-K1 | EC50 |
>10 μM
Compound: 7 (KB130015)
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Agonism of compound towards thyroid response element (TRAF beta) in CHO-K1 cells
Agonism of compound towards thyroid response element (TRAF beta) in CHO-K1 cells
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[PMID: 11806713] |
| CHO-K1 | IC50 |
2.2 μM
Compound: 7 (KB130015)
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Antagonism of compound towards thyroid response element (TRAF alpha) in CHO-K1 cells
Antagonism of compound towards thyroid response element (TRAF alpha) in CHO-K1 cells
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[PMID: 11806713] |
| CHO-K1 | IC50 |
4.1 μM
Compound: 7 (KB130015)
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Antagonism of compound towards thyroid response element (TRAF beta) in CHO-K1 cells
Antagonism of compound towards thyroid response element (TRAF beta) in CHO-K1 cells
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[PMID: 11806713] |
| CHO-K1 | IC50 |
4.5 μM
Compound: 7 (KB130015)
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Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells
Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells
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[PMID: 11806713] |
| CHO-K1 | IC50 |
5.1 μM
Compound: 7 (KB130015)
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Concentration required to inhibit 50% of binding of [125I]T3 to human Thyroid hormone receptor beta 1 in CHO-K1 cells
Concentration required to inhibit 50% of binding of [125I]T3 to human Thyroid hormone receptor beta 1 in CHO-K1 cells
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[PMID: 11806713] |
KB130015 (1-10 μM) slows the inactivation kinetics of cardiac Na+ channels by enhancing a slow-inactivating INa component at the expense of the fast-inactivating component in guinea pig, rabbit, and pig ventricular myocytes[2].
KB130015 shifts the steady-state voltage-dependent inactivation of Na+ channels to more negative potentials and slows the recovery from inactivation in cardiac myocytes[2].
KB130015 (10 μM) decreases the amplitude of L-type Ca2+current (Ica-L) by about 30% without changing its inactivation time course in pig ventricular myocytes[2].
KB130015 (50 μM) exerts a positive inotropic action by increasing cell shortening amplitude in pig ventricular myocytes without altering the time course[2].
KB130015 (100 μM) shortens the action potential duration (APD) in pig ventricular trabeculum but prolongs short APDs and induces early afterdepolarizations (EADs) in mouse left ventricular papillary muscle[2].
KB130015 (100 μM) activates large-conductance Ca2+-activated K+ (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells and the BKCa channels from insects (Drosophila melanogaster dSlo and Periplaneta americana pSlo) expressed in HEK 293 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KB130015 (30-300 mg/kg, p.o., daily, 2 weeks) alters thyroid hormone levels (reduces T3, increases T4 and TSH) in Sprague-Dawley rats[1].
KB130015 (20 mg/kg, i.p., daily, 20 days) suppresses ventricular premature beats, ventricular tachycardia and fibrillation during ischemia and reperfusion in rabbits with left anterior descending artery occlusion[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (each group consisting of 5 males and 5 females)[1]
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Dosage:30, 100, 300 mg/kg
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Administration:p.o. daily for 2 weeks
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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.
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Animal Model:Rabbits with ischemia and reperfusion were established by 30-min occlusion of the left anterior descending artery[2]
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Dosage:20 mg/kg
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Administration:i.p. daily for 20 days
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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.
Chemical Information
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CAS No. 147030-48-6
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Appearance Solid
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분자량 548.11
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화학식 C18H14I2O4
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Color Off-white to light yellow
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SMILES
O=C(COC1=C(C=C(C=C1I)CC2=C(OC3=C2C=CC=C3)C)I)O
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Synonyms
KB015
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Environ Sci Technol
IodoFinder: Machine Learning-Guided Recognition of Iodinated Chemicals in Nontargeted LC-MS/MS Analysis. [Abstract]2025 Mar 11;59(9):4530-4539. PMID: 40015982
용액&용해도
DMSO : 100 mg/mL (182.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
[3]. Gessner G, et al. The amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015) opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle. Eur J Pharmacol. 2007 Jan 26;555(2-3):185-93. [Content Brief]
[4]. Gessner G, et al. The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism. Eur J Pharmacol. 2010 Apr 25;632(1-3):52-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8245 mL | 9.1223 mL | 18.2445 mL | 45.6113 mL |
| 5 mM | 0.3649 mL | 1.8245 mL | 3.6489 mL | 9.1223 mL | |
| 10 mM | 0.1824 mL | 0.9122 mL | 1.8245 mL | 4.5611 mL | |
| 15 mM | 0.1216 mL | 0.6082 mL | 1.2163 mL | 3.0408 mL | |
| 20 mM | 0.0912 mL | 0.4561 mL | 0.9122 mL | 2.2806 mL | |
| 25 mM | 0.0730 mL | 0.3649 mL | 0.7298 mL | 1.8245 mL | |
| 30 mM | 0.0608 mL | 0.3041 mL | 0.6082 mL | 1.5204 mL | |
| 40 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL | 1.1403 mL | |
| 50 mM | 0.0365 mL | 0.1824 mL | 0.3649 mL | 0.9122 mL | |
| 60 mM | 0.0304 mL | 0.1520 mL | 0.3041 mL | 0.7602 mL | |
| 80 mM | 0.0228 mL | 0.1140 mL | 0.2281 mL | 0.5701 mL | |
| 100 mM | 0.0182 mL | 0.0912 mL | 0.1824 mL | 0.4561 mL |
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