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  1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Lesopitron dihydrochloride

Lesopitron dihydrochloride  (Synonyms: E4424)

目錄號: HY-101609 純度: ≥98.0%
COA 產(chǎn)品使用指南 技術(shù)支持

Lesopitron dihydrochloride 是選擇性的 5-HT1A 受體激動劑,作用于大鼠海馬膜,IC50 為 125 nM。

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Lesopitron dihydrochloride Chemical Structure

Lesopitron dihydrochloride Chemical Structure

CAS No. : 132449-89-9

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1 mg ¥2000
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Other Forms of Lesopitron dihydrochloride:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.

IC50 & Target

5-HT1A Receptor

125 nM (IC50, in rat hippocampal membranes)

體外研究
(In Vitro)

In vitro binding and autoradiographic studies with [3H]8-OH-DPAT and [3H]Lesopitron as radioligands confirm that Lesopitron binds to 5-HT1A receptors in the rat brain with a relatively high affinity (pKi=7.35). As expected of a full agonist at postsynaptic 5-HT1A receptors, Lesopitron (IC50=125 nM) inhibits forskolin-stimulated adenylate cyclase activity in rat hippocampal membranes to the same extent as 5-HT. Lesopitron inhibits the firing of serotoninergic neurons both in vitro (in brainstem slices, IC50=120 nM)[1].

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

體內(nèi)研究
(In Vivo)

Lesopitron inhibits the firing of serotoninergic neurons both in vivo (in chloral hydrate-anaesthetized rats, ID50=35 μg/kg i.v.)[1]. Lesopitron administered at a dose which induces anxiolytic behaviour in rats (30 μg/kg, i.p.) markedly reduces 5-HT levels (to 45% of the basal value) in cortical perfusates[2].

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

分子量

393.74

Formula

C15H23Cl3N6

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

來索吡瓊二鹽酸鹽

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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 : 12.5 mg/mL (31.75 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)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(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5397 mL 12.6987 mL 25.3975 mL
5 mM 0.5079 mL 2.5397 mL 5.0795 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲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儲存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲存時(shí),請?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

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)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(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: ≥98.0%

參考文獻(xiàn)
Animal Administration
[2]

Rats[2]
Male Wistar rats weighing 270-300 g, are used. Lesopitron is administered either through the dialysis probe (dissolved in artificial CSF) or i.p. (dissolved in 0.9% saline, 2 mL/kg body weight).

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

參考文獻(xiàn)

Lesopitron dihydrochloride 相關(guān)分類

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲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儲存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲存時(shí),請?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 2.5397 mL 12.6987 mL 25.3975 mL 63.4937 mL
5 mM 0.5079 mL 2.5397 mL 5.0795 mL 12.6987 mL
10 mM 0.2540 mL 1.2699 mL 2.5397 mL 6.3494 mL
15 mM 0.1693 mL 0.8466 mL 1.6932 mL 4.2329 mL
20 mM 0.1270 mL 0.6349 mL 1.2699 mL 3.1747 mL
25 mM 0.1016 mL 0.5079 mL 1.0159 mL 2.5397 mL
30 mM 0.0847 mL 0.4233 mL 0.8466 mL 2.1165 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:
Lesopitron dihydrochloride
目錄號:
HY-101609
需求量: