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  2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Lusaperidone

Lusaperidone  (Synonyms: R107474)

目錄號: HY-U00117 純度: 99.81%
COA 產(chǎn)品使用指南 技術(shù)支持

Lusaperidone (R107474) 是一種α2腎上腺素受體 (adrenergic receptor) 拮抗劑，對α2A和α2C的 Ki 值分別為0.13和0.15 nM。

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Lusaperidone Chemical Structure

Lusaperidone Chemical Structure

CAS No. : 214548-46-6

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查看 Adrenergic Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.

IC50 & Target

Ki: 0.13 nM (α2A adrenergic receptor), 0.15 nM (α2C adrenergic receptor)[1]
體外研究
(In Vitro)

Lusaperidone has subnanomolar affinity for α2A and α2C adrenergic receptor (Ki=0.13 and 0.15 nM, respectively) and shows nanomolar affinity for the hα2B adrenergic receptor and h5-HT7 receptors (Ki=1 and 5 nM, respectively). Lusaperidone interacts weakly (Ki values ranging between 81 and 920 nM) with dopamine-hD2L, -hD3 and -hD4, h5-HT1D-, h5-HT1F-, h5-HT2A-, h5-HT2C-, and h5-HT5A receptors. Lusaperidone, tested up to 10 μM, interacts only at micromolar concentrations or not at all with any of the other receptor or transporter binding sites tested in this study. Lusaperidone has been shown to reverse the clonidine-induced inhibition of cyclic AMP production mediated by human α2A and α2C adrenoceptors expressed in cell lines (Kb is 2.8 and 4.4 nM, respectively) and is a full antagonist on both receptor subtypes[1].

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

Lusaperidone occupies the α2A and α2C adrenergic receptor with an ED50 of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 after in vivo intravenous administration is very rapid; in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection[1].

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

359.42

Formula

C22H21N3O2
CAS 號
性狀

固體

顏色

White to light yellow

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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 3.45 mg/mL (9.60 mM; 超聲助溶 (<60°C); 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 2.7823 mL 13.9113 mL 27.8226 mL
5 mM 0.5565 mL 2.7823 mL 5.5645 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。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.81%

參考文獻
Animal Administration
[1]

Rats: Radio labeled Lusaperidone (24–28 GBq/μmol) is injected into the tail vein of diethyl ether anesthetized male Wistar rats (200–250 g). The rats received 30–40 MBq (injected at the start of the experiment) in 300 μL saline including 10% (v/v) ethanol. The rats are sacrificed by cervical dislocation at 5, 10, 20, and 30 min post injection under diethyl ether anesthesia. A blood sample is taken by cardiac puncture and selected tissues are rapidly dissected and weighed. The radioactivity is measured[1].

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

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。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(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 2.7823 mL 13.9113 mL 27.8226 mL 69.5565 mL
5 mM 0.5565 mL 2.7823 mL 5.5645 mL 13.9113 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：
Lusaperidone
目錄號：
HY-U00117
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