TC-G-1008

SKU: orb1302683

Description

TC-G-1008 (GPR39-C3) is a potent and selective agonist of the zinc-sensing receptor GPR39, demonstrating sub-nanomolar EC50 values for both human and rat orthologs. This compound is a valuable research tool for investigating GPR39's role in metabolic regulation, endocrine function, and neurological processes in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1621175-65-2
• MW: 418.9
• Purity: 99.54% (May vary between batches)
• Formula: C₁₈H₁₉ClN₆O₂S
• SMILES: CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(n1)-c1ccccn1
• Target: GHSR
• Solubility: DMSO:255 mg/mL (608.74 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.77 mM)

Bioactivity

• Target IC50:
  GPR139 (human):0.8 nM|GPR39 (rat):0.4 nM
• In Vivo:
  Rat and mouse plasma protein binding for TC-G-1008 is 99.3% and 99.1%, respectively. TC-G-1008 is the first potent GPR39 agonist (EC50s ≤ 1 nM for human and rat receptor) that is orally bioavailable in mice and significantly induces acute GLP-1 levels. Following single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves maximal exposures of 1.4, 6.1, and 25.3 μM, respectively, between 1 and 1.5 hours.
• In Vitro:
  TC-G-1008 demonstrates selectivity over a panel of kinases (IC50s>10 μM) and lacks significant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM). GPR39-C3 acts as a positive allosteric modulator in HEK293-GPR39 cells, activating cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment, and induces dose- and time-dependent loss of response in cAMP production upon second challenge.
• Animal Research:
  Mice: Mice are given single oral doses of 10, 30, and 100 mg/kg of TC-G-1008 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, hGPR39, GPR39-C3, Growth hormone secretagogue receptor, GHSR, GHS-R, rGPR39, TC G 1008, TC-G 1008, TCG1008, TC-G1008, TC-G-1008

Compound Identifiers

PubChem CID

91826086