| Name | SB 258719 |
| Description | SB 258719 is a selective antagonist of 5-HT7 receptor with pKi of 7.5. |
| In vitro | SB 258719 antagonised surmountably 5-CT-stimulated adenylyl cyclase activity. Schild analysis of the antagonism by SB 258719 gave a pA2 of 7.2±0.2 and slope not significantly different from 1, consistent with competitive antagonism[3]. |
| In vivo | SB 258719 (5-20 mg/kg, i.p.) reversed the hypothermic effect of 5-CT in mice[1], attenuated increased Wnt/β-catenin activity in HCC cell lines and patient-derived primary tumor tissues in the presence of 5-HT, and reduced tumor growth in vivo[2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (14.77 mM), Sonication is recommended. DMSO : 250 mg/mL (738.53 mM), Sonication is recommended.
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| Keywords | Serotonin Receptor | selective | SB-258719 | SB258719 | SB 258719 | partial | inverse | Inhibitor | inhibit | hydrochloride | apparent | agonism | affinity | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT7 receptor | 5-HT7 | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Sevoflurane | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | 1,8-Cineole | Dopamine hydrochloride | Cloperastine hydrochloride | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine | Doxepin hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Serotonin Receptor-Targeted Compound Library | Anti-Cancer Active Compound Library |