1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. SB 243213

SB 243213 是一种口服有效的,选择性的,高亲和力的 5-HT2C 受体拮抗剂,对人 5-HT2C 受体的 pKi 为 9.37,pKb 为 9.8。SB 243213 对多种神经递质受体、酶和离子通道具有超过 100 倍的选择性。SB 243213 具有改善的抗焦虑特性,有用于精神分裂症和运动障碍的潜力。

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SB 243213 Chemical Structure

SB 243213 Chemical Structure

CAS No. : 200940-22-3

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10 mM * 1 mL in DMSO ¥990
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5 mg ¥900
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10 mg ¥1500
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25 mg ¥3500
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Customer Review

Other Forms of SB 243213:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders[1].

IC50 & Target[1]

Human 5-HT2C Receptor

9.37 (pKi)

human 5-HT1A Receptor

<5.3 (pKi)

human 5-HT1B Receptor

5.5 (pKi)

human 5-HT1D Receptor

6.32 (pKi)

human 5-HT1E Receptor

<5.4 (pKi)

human 5-HT1F Receptor

5.35 (pKi)

Human 5-HT2A Receptor

7.01 (pKi)

human 5-HT2B Receptor

7.2 (pKi)

Human 5-HT6 Receptor

6.5 (pKi)

Human 5-HT7 Receptor

5.64 (pKi)

体外研究
(In Vitro)

SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=6.7) for the cloned human D2 receptor[1].

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

体内研究
(In Vivo)

SB 243213 (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box[1].
SB 243213 (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction[1].

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

Animal Model: Male Sprague-Dawley experimentally naive rats (220-300 g)[1]
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: PO; 1 hour pre-test
Result: Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
分子量

428.41

Formula

C22H19F3N4O2

CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (291.78 mM; 超声助溶; 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 2.3342 mL 11.6711 mL 23.3421 mL
5 mM 0.4668 mL 2.3342 mL 4.6684 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3342 mL 11.6711 mL 23.3421 mL 58.3553 mL
5 mM 0.4668 mL 2.3342 mL 4.6684 mL 11.6711 mL
10 mM 0.2334 mL 1.1671 mL 2.3342 mL 5.8355 mL
15 mM 0.1556 mL 0.7781 mL 1.5561 mL 3.8904 mL
20 mM 0.1167 mL 0.5836 mL 1.1671 mL 2.9178 mL
25 mM 0.0934 mL 0.4668 mL 0.9337 mL 2.3342 mL
30 mM 0.0778 mL 0.3890 mL 0.7781 mL 1.9452 mL
40 mM 0.0584 mL 0.2918 mL 0.5836 mL 1.4589 mL
50 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1671 mL
60 mM 0.0389 mL 0.1945 mL 0.3890 mL 0.9726 mL
80 mM 0.0292 mL 0.1459 mL 0.2918 mL 0.7294 mL
100 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5836 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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产品名称:
SB 243213
目录号:
HY-103112B
需求量: