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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Sobetirome (3,5-dimethyl-4[(4'-hydroxy-3'-isopropylbenzyl)-phenoxy] acetic acid, also known as GC-1 and QRX-431, is a member of a class of compounds known as selective thyromimetics.It was firstly developed by Thomas Scanlan’s group at the University of California-San Francisco (UCSF) in 1995 1.
In cholesterol-fed rats, sobetirome was shown to lower plasma cholesterol in a dose-dependent manner by up to 75% of untreated controls. In hypercholesterolemic mice, sobetirome was failed to induce LDL receptor mRNA expression. In different mouse models, sobetirome and T-0681 were shown to promote bile acid production and biliary sterol secretion. In cynomolgus monkeys, sobetirome was shown to reduce plasma cholesterol in a dose-dependent manner by up to 30%. Both sobetirome and T-0681 were shown to increase hepatic expression of the HDL receptor (scavenger receptor-BI, SR-BI) in animals.
In Phase I clinical trials, Sobetirome was shown to be generally well tolerated at all doses studied and proof of the therapeutic concept of cholesterol lowering was clearly demonstrated 1.
References:1. Tancevski I, Demetz E, Eller P. Sobetirome: a selective thyromimetic for the treatment of dyslipidemia. Recent Pat Cardiovasc Drug Discov. 2011 Jan;6(1):16-9.
Cell lines
Rat brown adipocytes.
Preparation method
Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reaction Conditions
0.2-200 nM; 24 h.
Applications
In rat brown adipocytes, GC-1 increases Ucp1 mRNA expression and D2 activity stimulated by adrenergic. Also, GC-1 (10 nM) further increases cAMP production induced by NE or BRL 37344.
Animal models
Hypothyroid mice.
Dosage form
1.8-49.33 ng/g BW. day; 4 weeks of daily ip injection.
In hypothyroid mice, GC-1 increases heart rate and maximum speeds of contraction (dP/dtmax). GC-1 increases dP/dtmax and arterial pressure by 17% and 39%, respectively.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Martinez de Mena R,Scanlan TS,Obregon MJ. The T3 receptor beta1 isoform regulates UCP1 and D2 deiodinase in rat brown adipocytes. Endocrinology, 2010, 151(10): 5074-5083.
[2]. Trost SU, Swanson E, Gloss B, et al. The thyroid hormone receptor-beta-selective agonist GC-1 differentially affects plasma lipids and cardiac activity. Endocrinology, 2000, 141(9): 3057-3064.
