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Submit ReviewAF 64394 is a potent and selective GPR3 inverse agonist (pIC50 = 7.3). Selective for GPR3 over GPR6 and GPR12 (pIC50 values are 5.1 and 4.9, respectively).
AF 64394 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 393.87 |
Formula | C21H20ClN5O |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1637300-25-4 |
PubChem ID | 125286314 |
InChI Key | WBYNZQXAAWPAGR-UHFFFAOYSA-N |
Smiles | CC(C)OC1=C(CNC2=CC(=NC3=NC=NN23)C2=CC=CC=C2)C=CC(Cl)=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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 39.39 | 100 |
The following data is based on the product molecular weight 393.87. 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.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.54 mL | 12.69 mL | 25.39 mL |
5 mM | 0.51 mL | 2.54 mL | 5.08 mL |
10 mM | 0.25 mL | 1.27 mL | 2.54 mL |
50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
References are publications that support the biological activity of the product.
Jensen et al (2014) The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function. Bioorg.Med.Chem.Lett. 24 5195 PMID: 25442311
Godlewski et al (2015) Mice lacking GPR3 receptors display late-onset obese phenotype due to impaired thermogenic function in brown adipose tissue. Sci.Rep. 5 14953 PMID: 26455425
If you know of a relevant reference for AF 64394, please let us know.
Keywords: AF 64394, AF 64394 supplier, AF64394, Potent, selective, GPR3, inverse, agonists, agonism, obesity, Orphan, 7-TM, Receptors, 6931, Tocris Bioscience
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