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

SB 243213 是一種口服有效的,選擇性的,高親和力的 5-HT2C 受體拮抗劑,對人 5-HT2C 受體的 pKi 為 9.37,pKb 為 9.8。SB 243213 對多種神經(jīng)遞質受體、酶和離子通道具有超過 100 倍的選擇性。SB 243213 具有改善的抗焦慮特性,有用于精神分裂癥和運動障礙的潛力。

MCE 的所有產品僅用作科學研究或藥證申報,我們不為任何個人用途提供產品和服務

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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10 mg ¥1500
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Customer Review

Other Forms of SB 243213:

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

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)

體外研究
(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.

體內研究
(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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 125 mg/mL (291.78 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 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
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內使用, -20°C儲存時,請在1年內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內使用, -20°C儲存時,請在1年內使用。

可選溶劑 濃度 溶劑體積 質量 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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產品名稱:
SB 243213
目錄號:
HY-103112B
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