GC-1 (Sobetirome) 100MCG

GC-1 (Sobetirome) 100MCG

GC-1 (Sobetirome) 100MCG

GC-1 (Sobetirome) 100MCG

GC-1 (Sobetirome) is a halogen-free, subtype-selective synthetic agonist of thyroid hormone receptor beta (TRβ1). Engineered as a targeted thyromimetic, GC-1 binds TRβ1 with high affinity (EC50 ≈ 0.15 nM), isolating hepatic lipid metabolism and thermogenic uncoupling pathways from TRα1-mediated cardiac activity. GC-1 upregulates hepatic LDL receptor expression, accelerates reverse cholesterol transport, and stimulates uncoupling protein 1 (UCP1) in adipose tissue.

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Certificate of Analysis

What is GC-1 (Sobetirome)?

GC-1 (known chemically as Sobetirome or 2-[4-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-3,5-dimethylphenoxy]acetic acid) is a pioneer halogen-free, subtype-selective synthetic thyromimetic. Developed to overcome the severe cardiotoxic limitations of non-selective thyroid hormones (such as triiodothyronine / T3 and thyroxine / T4), Sobetirome selectively targets thyroid hormone receptor beta (TRβ1) over thyroid hormone receptor alpha (TRα1).

Because TRβ1 receptors predominate in the liver and adipose tissue while TRα1 receptors govern cardiac pacemaker rate and myocardial oxygen consumption, GC-1 (Sobetirome) isolates beneficial hepatic lipid clearance, bile acid synthesis, and thermogenic energy expenditure pathways without inducing tachycardia, cardiac hypertrophy, or muscle catabolism.

Batch-verified for high analytical purity at Modern Aminos, GC-1 (Sobetirome) is offered as a standardized reference material for cell culture and biochemical research. Researchers evaluating hepatic lipid turnover, reverse cholesterol transport, and brown adipose tissue (BAT) thermogenesis utilize GC-1 alongside complementary metabolic reference standards available on the site, such as SLU-PP-332, BAM15, GW-501516 (Cardarine), and AICAR.

Chemical and Molecular Data

Compound Name GC-1 (Sobetirome)
Quantity / Formats Offered High-Purity Dry Reference Powder / Solid Unit Material
Chemical Structure Selective Non-Halogenated Phenoxyacetic Acid Thyromimetic
Synonyms / Alt Names Sobetirome, GC-1, QR-440, TRβ-Selective Agonist GC-1
CAS Number 211159-22-4
Chemical Formula C20H24O4
Molecular Weight 328.40 g/mol
IUPAC Name 2-[4-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-3,5-dimethylphenoxy]acetic acid
InChIKey InChIKey=GZAYDGSXQVMEGT-UHFFFAOYSA-N
SMILES Code CC(C)C1=C(C=CC(=C1)CC2=C(C=C(C=C2C)OCC(=O)O)C)O

What are the Mechanisms of Action?

The biochemical pathways and cellular targets include:

  • Selective TRβ1 Receptor Agonism over TRα1: GC-1 binds TRβ1 with high affinity (EC50 ≈ 0.15 nM), displaying over 10-fold higher binding selectivity and up to 40-fold greater functional transactivation potency for TRβ1 compared to TRα1. This prevents cardiac activation while fully stimulating hepatic thyroid response elements (TREs).
  • Hepatic LDL Receptor Upregulation & Reverse Cholesterol Transport: In hepatocyte cell lines, GC-1 (Sobetirome) stimulates transcription of low-density lipoprotein receptors (LDLR) and cholesterol 7α-hydroxylase (CYP7A1). This accelerates circulating LDL-cholesterol uptake and drives conversion of hepatic cholesterol into bile acids for excretion.
  • Adipose Thermogenesis & UCP1 Induction: Sobetirome acts directly on brown adipose tissue (BAT) and white adipose tissue (WAT) to upregulate Uncoupling Protein 1 (UCP1) gene expression. Uncoupling electron transport from ATP synthesis converts mitochondrial proton gradients into heat, elevating basal energy expenditure.

What do Preclinical & Academic Studies Show for GC-1 (Sobetirome)?

When evaluating research efficacy and published scientific literature:

  • Subtype Selectivity & Metabolic Clearance (PubMed): Landmark bioenergetic studies cataloged on PubMed (PMID: 10080779) confirm that GC-1 (Sobetirome) significantly lowers plasma cholesterol and triglycerides in hyperlipidemic models without elevating heart rate or inducing cardiac remodeling.
  • Hepatic Steatosis & Thermogenic Uncoupling (PMC): Comprehensive biomedical reviews archived in PMC (PMC2831526) document Sobetirome’s capacity to reduce hepatic triglyceride accumulation, enhance fatty acid oxidation, and stimulate WAT browning in metabolic disease research.
  • Chemical Profiling & Identification (PubChem): Official structural characterization maintained on PubChem verifies the molecular mass (328.40 g/mol), non-halogenated phenoxyacetic acid structure, and HPLC mass spectrometry profile of CAS 211159-22-4.

How does GC-1 (Sobetirome) compare to other compounds?

To evaluate thyroid receptor subtype selectivity, metabolic pathways, and mitochondrial targets, researchers compare GC-1 against alternative reference standards available at Modern Aminos:

GC-1 (Sobetirome) vs. Non-Selective T3 / T4 Thyroid Hormones

In metabolic and endocrine research, receptor subtype selectivity dictates tissue specificity:

  • GC-1 (Sobetirome): Subtype-selective TRβ1 agonist. Selectively drives hepatic lipid clearance, CYP7A1 bile acid conversion, and adipose UCP1 thermogenesis while sparing cardiac TRα1 receptors, eliminating thyrotoxic heart rate spikes.
  • Endogenous T3 / T4 Hormones: Non-selective agonists that bind TRα1 and TRβ1 with equal affinity. While effective at stimulating basal metabolic rate, non-selective TRα1 stimulation induces severe cardiac side effects, muscle wasting, and bone mineral density loss.
Compound / Reference Chemical Structure & Class Core Mechanism of Action Research Focus & Profile
GC-1 (Sobetirome) Halogen-Free TRβ-Selective Thyromimetic Agonizes TRβ1 to upregulate hepatic LDLR/CYP7A1 and adipose UCP1 without cardiac TRα1 activation Focuses on tissue-selective lipid lowering, hepatic steatosis clearance, reverse cholesterol transport, and BAT thermogenesis
SLU-PP-332 Pan-ERR Nuclear Receptor Agonist Binds ERRα/β/γ to recruit PGC-1α and upregulate mitochondrial OXPHOS gene networks Focuses on nuclear receptor exercise mimetics, oxidative muscle fiber switching, and de novo mitochondrial biogenesis
BAM15 Mitochondrial Protonophore Uncoupler Discharges the inner mitochondrial membrane proton gradient to uncouple oxidative phosphorylation from ATP synthesis Focuses on nutrient burning, energy expenditure elevation, and lipid oxidation independent of nuclear hormone receptors
GW-501516 (Cardarine) PPARδ Selective Agonist Recruits PGC-1α via PPARδ to upregulate skeletal muscle fatty acid beta-oxidation and PDK4 expression Focuses on PPARδ nuclear receptor signaling, fatty acid transport (FAT/CD36), and glycogen sparing in myocytes

Frequently Asked Questions (FAQs)

1. Is Modern Aminos a reliable place to buy GC-1 (Sobetirome)?

Yes, Modern Aminos is a highly trusted vendor for high-purity research chemicals and reference compounds. Every batch of GC-1 (Sobetirome) undergoes strict third-party analytical testing (including HPLC and Mass Spectrometry) to verify minimum 98%+ chemical purity, correct molecular weight (328.40 g/mol), exact TRβ selectivity parameters, and complete absence of heavy metals or synthesis impurities.

2. What is GC-1 (Sobetirome) and how is it classified chemically?

GC-1 (Sobetirome) is a halogen-free synthetic phenoxyacetic acid derivative. It is classified chemically as a subtype-selective thyroid hormone receptor beta (TRβ1) agonist designed to isolate hepatic lipid metabolism from cardiotoxic TRα signaling.

3. How does TRβ selectivity differ from TRα activation in metabolic models?

TRβ1 receptors predominate in hepatocytes and adipose tissue, regulating cholesterol breakdown, bile acid synthesis, and fatty acid oxidation. TRα1 receptors govern cardiac tissue rhythm and rate. Selective TRβ agonists like GC-1 drive metabolic lipid lowering without elevating heart rate or causing cardiac hypertrophy.

4. What role does GC-1 play in hepatic lipid clearance and cholesterol regulation?

In liver cell models, GC-1 upregulates low-density lipoprotein receptor (LDLR) expression and stimulates cholesterol 7α-hydroxylase (CYP7A1). This increases hepatic LDL-cholesterol clearance from circulation and accelerates conversion of cholesterol into bile acids.

5. How does Sobetirome induce thermogenesis and white adipose tissue browning?

GC-1 binds TRβ receptors in adipose tissue to stimulate transcription of Uncoupling Protein 1 (UCP1). UCP1 uncouples mitochondrial electron transport from ATP production, converting energy into heat and promoting a brown-like oxidative phenotype in white adipocytes.

6. How does GC-1 compare to BAM15 or SLU-PP-332 in metabolic assays?

GC-1 is a thyroid nuclear receptor agonist targeting TRβ1. SLU-PP-332 targets Estrogen-Related Receptors (ERRs) to promote oxidative muscle fiber switching. BAM15 is a chemical protonophore that directly uncouples mitochondrial respiration without nuclear receptor binding.

7. How does Modern Aminos verify the chemical purity and identity of GC-1?

Modern Aminos utilizes High-Performance Liquid Chromatography (HPLC) to confirm active chemical purity exceeding 98% and Mass Spectrometry (MS) to verify exact molecular weight (328.40 g/mol) and structural identity prior to batch release.

8. What are the recommended storage parameters for GC-1 reference standards?

GC-1 (Sobetirome) reference material should be stored tightly sealed in a cool, dry environment (15°C to 25°C) or refrigerated for long-term preservation. Protect from direct heat, light exposure, and atmospheric moisture to maintain solid-state chemical stability.

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