TC-G 1008

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Cat.No. 5355 - TC-G 1008 | C18H19ClN6O2S | CAS No. 1621175-65-2
Description: Potent and selective GPR39 agonist
Chemical Name: N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

Potent and selective GPR39 agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). Selective over a panel of kinases (IC50s > 10 μM) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50s > 30 μM). Increases GLP-1 levels in vitro and in vivo. Orally bioavailable.

Compound Libraries

TC-G 1008 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 418.9
Formula C18H19ClN6O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1621175-65-2
PubChem ID 91826086
InChI Key DRSZMILOMUPIBJ-UHFFFAOYSA-N
Smiles CNC1=NC(NCC2=C(Cl)C=C(NS(C)(=O)=O)C=C2)=CC(C3=NC=CC=C3)=N1

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

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.89 100

Preparing Stock Solutions

The following data is based on the product molecular weight 418.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.39 mL 11.94 mL 23.87 mL
5 mM 0.48 mL 2.39 mL 4.77 mL
10 mM 0.24 mL 1.19 mL 2.39 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Peukert et al (2014) Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 5 1114 PMID: 25313322


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Keywords: TC-G 1008, supplier, TC-G1008, potent, selective, GPR39, agonists, agonism, Orphan, 7-TM, Receptors, Orphan, 7-TM, Receptors, Tocris Bioscience

1 Citation for TC-G 1008

Citations are publications that use Tocris products. Selected citations for TC-G 1008 include:

Mlyniec et al (2016) Potential antidepressant-like properties of the TC G-1008, a GPR39 (zinc receptor) agonist. J Affect Disord. 201 179 PMID: 27235821


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