Biological Activity
Reversible corticotropin releasing factor receptor 1 (CRF1) antagonist (Ki values are 3.4 and 7.9 nM at rat and human CRF1 respectively) that displays >1000-fold selectivity over CRF2 receptors. Suppresses CRF-induced ACTH release in vitro (IC50 = 241 nM) and is brain penetrant.
Technical Data
| M. Wt | 355.43 |
| Formula | C19H25N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 197801-88-0 |
| PubChem ID | 10291750 |
| InChI Key | FZMBHAQCHCEGNN-UHFFFAOYSA-N |
| Smiles | CCC(COC)N2C1=CC(C)=NC(NC3=CC=C(OC)C=C3C)=C1N=N2 |
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 | 35.54 | 100 | |
| ethanol | 35.54 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 355.43. 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 | 2.81 mL | 14.07 mL | 28.13 mL |
| 5 mM | 0.56 mL | 2.81 mL | 5.63 mL |
| 10 mM | 0.28 mL | 1.41 mL | 2.81 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kumar et al (2006) Synthesis and in vivo evaluation of [11C]SN003 as a PET ligand for CRF1 receptors. Bioorg.Med.Chem. 14 4029 PMID: 16529935
Sullivan et al (2007) PET imaging of CRF1 with [11C]R121920 and [11C]DMP696: Is the target of sufficient density? Nucl.Med.Biol 34 353 PMID: 17499724
Zhang et al (2003) Pharmacological characterization of a novel nonpeptide antagonist radioligand, (±)-N-[2-Methyl-4-methoxyphenyl]-1-(1-(methoxymethyl) propyl)-6-methyl-1H-1,2,3-triazolo[4,5-c]pyridin-4-amine ([3H]SN003) for cortic J.Pharm.Exp.Ther. 305 57 PMID:
Keywords: SN 003, supplier, reversible, corticotropin, releasing, factor, receptors, 1, CRF1, CRF, antagonists, SN003, CRF1, Receptors, CRF1, Receptors, Tocris Bioscience
