Biological Activity
Potent and selective 5-HT7 receptor antagonist (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B and < 6.0 for 5-HT1A, 5-HT1D, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT4 and 5-HT6 receptors respectively). Brain penetrant in vivo.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline.
Compound Libraries
SB 269970 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 388.95 |
Formula | C18H28N2O3S.HCl |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 261901-57-9 |
PubChem ID | 11957684 |
InChI Key | XQCJOYZLWFNDIO-PKLMIRHRSA-N |
Smiles | OC1=CC(S(N2[C@@H](CCN3CCC(C)CC3)CCC2)(=O)=O)=CC=C1.Cl |
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 | |||
phosphate buffered saline | 1.76 | 5 | |
DMSO | 38.89 | 100 | |
water | 7.78 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 388.95. 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 | 2.57 mL | 12.86 mL | 25.71 mL |
5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
10 mM | 0.26 mL | 1.29 mL | 2.57 mL |
50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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References
References are publications that support the products' biological activity.
Hagan et al (2000) Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist. Br.J.Pharmacol. 130 539 PMID: 10821781
Kogan et al (2002) DR4004, a putative 5-HT7 receptor antagonist, also has functional activity at the dopamine receptor. Eur.J.Pharmacol. 449 105 PMID: 12163113
Lovell et al (2000) A novel, potent, and selective 5-HT7 antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)-ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970) J.Med.Chem. 43 342 PMID: 10669560
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