1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB-215505

SB-215505 是一种有效的,亚型选择性 5-HT2B 受体拮抗剂,对 5-HT2B,5-HT2A,5-HT2CpKi 值分别为 8.3、6.77、7.66。SB-215505 可以增加大鼠的清醒和运动活动。

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SB-215505 Chemical Structure

SB-215505 Chemical Structure

CAS No. : 162100-15-4

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1 mg ¥1960
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5 mg ¥4830
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively[1]. SB-215505 increases wakefulness and motor activity in rats[2].

IC50 & Target[1]

5-HT2B Receptor

8.3 (pKi)

5-HT2A Receptor

6.77 (pKi)

5-HT2C Receptor

7.66 (pKi)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 IC50
13 nM
Compound: SB-215505
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay
[PMID: 19307114]
CHO-K1 IC50
64 nM
Compound: SB-215505
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin
[PMID: 19307114]
体外研究
(In Vitro)

SB-215505 is 30 fold selective for the 5-HT2B over the 5-HT2A receptor, and only marginally selective over the 5-HT2C receptor[1].

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

体内研究
(In Vivo)

SB-215505 (0.1-1.0 mg/kg; i.p.; two doses) dose-dependently increases wakefulness (W) and decreases IS, PS, SWS-2[2].

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

Animal Model: Male Sprague-Dawley rats weighing 230-260 g[2]
Dosage: 0.1, 0.3 and 1.0 mg/kg
Administration: IP; two doses (4 days between two doses)
Result: Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.
分子量

337.80

Formula

C19H16ClN3O

CAS 号
性状

固体

颜色

Off-white to light brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (74.01 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9603 mL 14.8017 mL 29.6033 mL
5 mM 0.5921 mL 2.9603 mL 5.9207 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9603 mL 14.8017 mL 29.6033 mL 74.0083 mL
5 mM 0.5921 mL 2.9603 mL 5.9207 mL 14.8017 mL
10 mM 0.2960 mL 1.4802 mL 2.9603 mL 7.4008 mL
15 mM 0.1974 mL 0.9868 mL 1.9736 mL 4.9339 mL
20 mM 0.1480 mL 0.7401 mL 1.4802 mL 3.7004 mL
25 mM 0.1184 mL 0.5921 mL 1.1841 mL 2.9603 mL
30 mM 0.0987 mL 0.4934 mL 0.9868 mL 2.4669 mL
40 mM 0.0740 mL 0.3700 mL 0.7401 mL 1.8502 mL
50 mM 0.0592 mL 0.2960 mL 0.5921 mL 1.4802 mL
60 mM 0.0493 mL 0.2467 mL 0.4934 mL 1.2335 mL
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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Inquiry Information

产品名称:
SB-215505
目录号:
HY-18596
需求量: