SB 258719 hydrochloride

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SB 258719 hydrochloride 

SB 258719 hydrochloride 是一种选择性的 5-HT7 受体拮抗剂,与该受体亲和度高(pKi=7.5)。SB-258719 hydrochloride 可以用于癌症和神经系统疾病的研究 。

SB 258719 hydrochloride

SB 258719 hydrochloride Chemical Structure

CAS No. : 1217674-10-6

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SB 258719 hydrochloride 的其他形式现货产品:

SB 258719

生物活性

SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases[1][2].

IC50 & Target[1]

5-HT7 Receptor

7.5 (pKi)

体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SB-258719 (5~20 mg/kg; i.p.) hydrochloride significantly attenuates the 5-CT-induced hypothermia[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Swiss Webster mice (20~25 g)[2].
Dosage: 5~20 mg/kg
Administration: I.p.
Result: Significantly attenuated the 5-CT-induced hypothermia.

分子量

374.97

Formula

C18H31ClN2O2S

CAS 号

1217674-10-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Thomas DR, et al. Functional characterisation of the human cloned 5-HT7 receptor (long form); antagonist profile of SB-258719. Br J Pharmacol. 1998;124(6):1300-1306.

    [2]. Guscott MR, et al. The hypothermic effect of 5-CT in mice is mediated through the 5-HT7 receptor. Neuropharmacology. 2003;44(8):1031-1037.

    [3]. Fatima S, et al. 5-Hydroxytryptamine promotes hepatocellular carcinoma proliferation by influencing β-catenin. Mol Oncol. 2016;10(2):195-212.

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