SB 258719

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB 258719 是 5-HT7 受体的选择性拮抗剂，pKi 为 7.5。

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.(In Vivo):SB 258719 (5-20 mg/kg, i.p.) reversed the hypothermic effect of 5-CT in mice. Increased Wnt/β-catenin activity was attenuated by SB 258719 in HCC cell lines and patient-derived primary tumour tissues in the presence of 5-HT. SB 258719 also reduced tumour growth in vivo.

SB 258719 (1, 3 and 10 μM; HEK 293 cells) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no signifcant alteration in the maximal response to 5-CT.

SB 258719 (5-20 mg/kg; i.p.) significantly attenuates the 5-CT-induced hypothermia. Animal Model:Male Swiss Webster mice (20-25 g).Dosage:5-20 mg/kg Administration:I.p.Result:Significantly attenuated the 5-CT-induced hypothermia.

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Endocrinology/Hormones

5-HT Receptor

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195199-95-2

338.51

C18H30N2O2S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (738.53 mM)

C[C@H](CCN1CCC(C)CC1)N(C)S(=O)(=O)c1cccc(C)c1

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(-20℃)

With Ice Pack

≥ 2 years