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KB130015

CAT: 0804-HY-120026-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-120026-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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[1][2][3][4].
CAS Number
147030-48-6
Product Name Alternative
KB015
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Calcium Channel; Potassium Channel; Sodium Channel; Thyroid Hormone Receptor
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling; Vitamin D Related/Nuclear Receptor
Applications
Neuroscience-Neuromodulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/kb130015.html
Purity
98.45
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(COC1=C(C=C(C=C1I)CC2=C(OC3=C2C=CC=C3)C)I)O
Molecular Formula
C18H14I2O4
Molecular Weight
548.11
Precautions
H302, H315, H319, H335
References & Citations
[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.|[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported