Sobetirome
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.
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 328.4 |
| Cas No. | 211110-63-3 |
| Formula | C20H24O4 |
| Synonyms | GC-1; QRX-431 |
| Solubility | ≥32.8 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥47.6 mg/mL in EtOH with ultrasonic |
| Chemical Name | 2-[4-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-3,5-dimethylphenoxy]acetic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=CC(=C1CC2=CC(=C(C=C2)O)C(C)C)C)OCC(=O)O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Rat brown adipocytes. |
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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. |
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Reaction Conditions |
0.2-200 nM; 24 h. |
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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 experiment [2]: | |
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Animal models |
Hypothyroid mice. |
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Dosage form |
1.8-49.33 ng/g BW. day; 4 weeks of daily ip injection. |
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Applications |
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. |
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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. |
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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. |
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| Description | Sobetirome(GC-1, QRX-431) is an agonist of thyroid hormone beta-receptor. | |||||
| Targets | thyroid hormone beta-receptor | |||||
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