Biological Activity
Potent and selective non-peptide NK3 receptor antagonist (Ki values are 4.4, > 100,000 and 250 nM for human NK3, NK1 and NK2 receptors respectively). Antihypertensive in vivo. Brain penetrant.
Licensing Information
Sold under license
Compound Libraries
SB 222200 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 380.48 |
| Formula | C26H24N2O |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 174635-69-9 |
| PubChem ID | 6604009 |
| InChI Key | MQNYRKWJSMQECI-QFIPXVFZSA-N |
| Smiles | O=C(C2=C(C)C(C4=CC=CC=C4)=NC3=CC=CC=C23)N[C@@H](CC)C1=CC=CC=C1 |
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
| Solubility | Soluble to 100 mM in DMSO and to 100 mM in ethanol |
Preparing Stock Solutions
The following data is based on the product molecular weight 380.48. 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 | 2.63 mL | 13.14 mL | 26.28 mL |
| 5 mM | 0.53 mL | 2.63 mL | 5.26 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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References
References are publications that support the products' biological activity.
Medhurst et al (1997) In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br.J.Pharmacol. 122 469 PMID: 9351503
Sarau et al (2000) Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J.Pharmacol.Exp.Ther. 295 373 PMID: 10992004
De Brito Gariepy and Couture (2010) Blockade of tachykinin NK3 receptor reverses hypertension through a dopaminergic mechanism in the ventral tegmental area of spontaneously hypertensive rats. Br.J.Pharmacol. 161 1868 PMID: 20804497
Keywords: SB 222200, supplier, Potent, selective, non-peptide, NK3, antagonists, Brain, penetrant, Tachykinin, Receptors, Neurokinin, SB222200, NK3, Receptor, NK3, Receptor, Tocris Bioscience
