TC-G 1005

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Description: Potent and selective GPBA receptor (TGR5) agonist
Chemical Name: (4-Cyclopropyl-3,4-dihydro-1(2H)-quinoxalinyl)[4-(2,5-dimethylphenoxy)-3-pyridinyl]methanone
Purity: ≥98% (HPLC)
Citations (1)
Pathways (1)

Biological Activity for TC-G 1005

TC-G 1005 is a potent and selective GPBA agonist (EC50 values are 0.72 nM and 6.2 nM for hTGR5 and mTGR5, respectively). TC-G 1005 is selective for TGR5 over FXR (farnesoid X receptor). TC-G 1005 increases plasma GLP-1 levels and reduces blood glucose in mice. Orally bioavailable.

Compound Libraries for TC-G 1005

TC-G 1005 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for TC-G 1005

M. Wt 399.48
Formula C25H25N3O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1415407-60-1
PubChem ID 71450251
Smiles CC1=CC(OC2=CC=NC=C2C(N3C(C=CC=C4)=C4N(C5CC5)CC3)=O)=C(C)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TC-G 1005

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 39.95 100
ethanol 39.95 100

Preparing Stock Solutions for TC-G 1005

The following data is based on the product molecular weight 399.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.5 mL 12.52 mL 25.03 mL
5 mM 0.5 mL 2.5 mL 5.01 mL
10 mM 0.25 mL 1.25 mL 2.5 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets for TC-G 1005

Certificate of Analysis / Product Datasheet
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References for TC-G 1005

References are publications that support the biological activity of the product.

Duan et al (2012) Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J.Med.Chem. 55 10475 PMID: 23148522

Urso et al (2020) Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am.J.Physiol.Lung Cell.Mol.Physiol. 318 L264 PMID: 31800261

If you know of a relevant reference for TC-G 1005, please let us know.

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Keywords: TC-G 1005, TC-G 1005 supplier, TC-G1005, TGR5, agonists, agonism, GLP-1, GPBA, glucose, bile, acid, receptors, bioavailable, TCG1005, Receptors, 5129, Tocris Bioscience

1 Citation for TC-G 1005

Citations are publications that use Tocris products. Selected citations for TC-G 1005 include:

Urso et al (2020) Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am.J.Physiol.Lung Cell.Mol.Physiol. 318 L264 PMID: 31800261

Do you know of a great paper that uses TC-G 1005 from Tocris? Please let us know.

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Pathways for TC-G 1005

Insulin Signaling Pathway

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.