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  2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. SB-200646A

SB-200646A 是第一個(gè)對(duì) 5-HT2B/2C 的選擇性超過(guò) 5-HT2A 的拮抗劑，5-HT2B，5-HT2C 和 5-HT2A 的 pKi 值分別為 7.5、6.9 和 5.2。SB-200646A 具有口服活性，在體內(nèi)具有電生理和抗焦慮特性。

在相同的摩爾濃度下，化合物鹽形式與游離形式有相同的生物活性，但鹽形式 SB-200646 通常具有更好的水溶性和穩(wěn)定性。

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SB-200646A Chemical Structure

SB-200646A Chemical Structure

CAS No. : 143797-62-0

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Customer Review

Other Forms of SB-200646A:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].

IC50 & Target[1][2]

5-HT2B Receptor

7.5 (pKi)

5-HT2C Receptor

6.9 (pKi)

5-HT2A Receptor

5.2 (pKi)

體外研究
(In Vitro)

SB200646A (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons[1].
The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons[1].

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

Animal Model: Male albino Sprague-Dawley rats (200-225 g at the beginning of treatment and 300-350 g at the time of the experiment)[1]
Dosage: 20 mg/kg
Administration: Intravenous injection; daily; for 21 days
Result: Significantly decreased the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons.
分子量

302.76

Formula

C15H15ClN4O
CAS 號(hào)
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 250 mg/mL (825.74 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.3029 mL 16.5147 mL 33.0295 mL
5 mM 0.6606 mL 3.3029 mL 6.6059 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3029 mL 16.5147 mL 33.0295 mL 82.5737 mL
5 mM 0.6606 mL 3.3029 mL 6.6059 mL 16.5147 mL
10 mM 0.3303 mL 1.6515 mL 3.3029 mL 8.2574 mL
15 mM 0.2202 mL 1.1010 mL 2.2020 mL 5.5049 mL
20 mM 0.1651 mL 0.8257 mL 1.6515 mL 4.1287 mL
25 mM 0.1321 mL 0.6606 mL 1.3212 mL 3.3029 mL
30 mM 0.1101 mL 0.5505 mL 1.1010 mL 2.7525 mL
40 mM 0.0826 mL 0.4129 mL 0.8257 mL 2.0643 mL
50 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6515 mL
60 mM 0.0550 mL 0.2752 mL 0.5505 mL 1.3762 mL
80 mM 0.0413 mL 0.2064 mL 0.4129 mL 1.0322 mL
100 mM 0.0330 mL 0.1651 mL 0.3303 mL 0.8257 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(chǎn)品名稱(chēng)：
SB-200646A
目錄號(hào)：
HY-103129
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