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Submit ReviewSB 222200 is a 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.
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SB 222200 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 100 | ||
ethanol | 100 |
The following data is based on the product molecular weight 380.48. 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 | 2.63 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 |
References are publications that support the biological activity of the product.
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 DArgic mechanism in the ventral tegmental area of spontaneously hypertensive rats. Br.J.Pharmacol. 161 1868 PMID: 20804497
If you know of a relevant reference for SB 222200, please let us know.
Keywords: SB 222200, SB 222200 supplier, Potent, selective, non-peptide, NK3, antagonists, Brain, penetrant, Tachykinin, Receptors, Neurokinin, SB222200, Receptor, 1393, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for SB 222200 include:
Stein et al (2009) Eosinophils utilize multiple chemokine receptors for chemotaxis to the parasitic nematode Strongyloides stercoralis. J Innate Immun 1 618 PMID: 20375616
Gallopin et al (2006) Cortical sources of CRF, NKB, and CCK and their effects on pyramidal cells in the neocortex. Mol Cancer 16 1440 PMID: 16339088
Do you know of a great paper that uses SB 222200 from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.