AF 64394

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Cat.No. 6931 - AF 64394 | C21H20ClN5O | CAS No. 1637300-25-4
Description: Potent and selective GPR3 inverse agonist
Chemical Name: N-[[4-Chloro-2-(1-methylethoxy)phenyl]methyl]-5-phenyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

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).

Technical Data

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.39 100

Preparing Stock Solutions

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

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References

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


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Citations for AF 64394

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