1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB-269970

SB-269970 是一种有效、选择性和可透过血脑屏障的 5-HT7 受体拮抗剂,pKi 为 8.3,对 5-HT7 受体选择性大于其他 5-HT 受体。

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SB-269970 Chemical Structure

SB-269970 Chemical Structure

CAS No. : 201038-74-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors[1][2].

IC50 & Target

Human 5-HT7 Receptor

8.3 (pKi)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
3.71 nM
Compound: SB-269970
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay
[PMID: 27475109]
体内研究
(In Vivo)

SB-269970 (3-30 mg/kg; i.p.; once) significantly blocks amphetamine and ketamine-induced hyperactivity[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL6/J mice[2]
Dosage: 3, 10, 30 mg/kg
Administration: Intraperitoneal injection; once
Result: Significantly blocked amphetamine and ketamine-induced hyperactivity.
分子量

352.49

Formula

C18H28N2O3S

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
SB-269970
目录号:
HY-15370
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