Chemical Name: (7S)-6-(Cyclopropylmethyl)-2-(2,4-dichlorophenyl)-7-ethyl-7,8-dihydro-4-methyl-6H-1,3,6,8a-tetraazaacenaphthylene hydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective corticotropin-releasing factor receptor 1 (CRF1) antagonist (Ki values are 4 and > 10000 nM at CRF1 and CRF2 respectively). Inhibits cAMP accumulation and adrenocorticotropic hormone (ACTH) production in vitro (pIC50 values are 7.1 and 6.9 respectively) and attenuates CRF and ACTH production in vivo. Orally active and brain penetrant with anxiolytic activity.
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
43.78
100
water
43.78
100
Preparing Stock Solutions
The following data is based on the product molecular weight 437.79. 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
2.28 mL
11.42 mL
22.84 mL
5 mM
0.46 mL
2.28 mL
4.57 mL
10 mM
0.23 mL
1.14 mL
2.28 mL
50 mM
0.05 mL
0.23 mL
0.46 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Millionet al (2003) A novel water-soluble selective CRF1 receptor antagonist, NBI 35965, blunts stress-induced visceral hyperalgesia and colonic motor function in rats. Brain Res. 985 32 PMID: 12957366
Hoareet al (2003) Mechanism of corticotropin-releasing factor type I receptor regulation by non-peptide antagonists. Mol.Pharmacol. 63 751 PMID: 12606786
Grosset al (2005) Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists. J.Med.Chem. 48 5780 PMID: 16134945