TC-G 1008
Tocris Bioscience, part of Bio-Techne | Catalog # 5355
Potent and selective GPR39 agonist
Key Product Details
Description
Potent and selective GPR39 agonist
Product Description
TC-G 1008 is a 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. Reduces TNF-α-induced oxidative stress, mitochondrial dysfunction, cytokine expression and secretion of MMPs in fibroblast-like synoviocytes (FLS). Orally bioavailable.Product Specifications
Molecular Weight
418.90
Formula
C18H19ClN6O2S
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
N-[3-Chloro-4-[[[2-(methylamino)-6-(2-pyridinyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.89 | 100 |
Preparing Stock Solutions
for TC-G 1008
The following data is based on the product molecular weight 418.90
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Jing The protective effects of the GPR39 agonist TC-G 1008 against TNF-α-induced inflammation in human fibroblast-like synoviocytes (FLSs). Eur J Pharmacol 2019 PMID: 31539553
- Peukert Discovery of 2-pyridylpyrimidines as the first orally bioavailable GPR39 agonists. ACS Med.Chem.Lett. 2014 PMID: 25313322
Product Specific Notices for TC-G 1008
For research use only
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