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  1. Neuronal Signaling Membrane Transporter/Ion Channel
  2. Cholinesterase (ChE) TRP Channel
  3. Imperatorin

Imperatorin  (Synonyms: 歐前胡素; Ammidin)

目錄號: HY-N0285 純度: 98.72%
COA 產(chǎn)品使用指南 技術(shù)支持

Imperatorin 是一種有效的 NO synthesis 抑制劑,IC50 為 9.2 μmol,也是 BChE 抑制劑,IC50 為 31.4 μmol。Imperatorin 是 TRPV1 的微弱激動劑,EC50 為 12.6±3.2 μM。

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Imperatorin Chemical Structure

Imperatorin Chemical Structure

CAS No. : 482-44-0

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10 mM * 1 mL in DMSO ¥550
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25 mg ¥500
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50 mg ¥800
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100 mg ¥1300
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Other Forms of Imperatorin:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

查看 Cholinesterase (ChE) 亞型特異性產(chǎn)品:

查看 TRP Channel 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

Imperatorin is an effective of NO synthesis inhibitor (IC50=9.2 μmol), which also is a BChE inhibitor (IC50=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC50 of 12.6±3.2 μM.

IC50 & Target

AChE

 

BChE

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 20 μg/mL
Compound: 13
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 29975532]
HepG2 IC50
> 20 μg/mL
Compound: 13
Cytotoxicity against human HepG2 cells by MTT assay
Cytotoxicity against human HepG2 cells by MTT assay
[PMID: 29975532]
MDA-MB-231 IC50
> 20 μg/mL
Compound: 13
Cytotoxicity against human MDA-MB-231 cells by MTT assay
Cytotoxicity against human MDA-MB-231 cells by MTT assay
[PMID: 29975532]
Neutrophil IC50
> 10 μM
Compound: 15
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins
[PMID: 24798144]
Neutrophil IC50
> 10 μM
Compound: 13
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release preincubated for 5 mins followed by fMLP/CB stimulation and measured for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release preincubated for 5 mins followed by fMLP/CB stimulation and measured for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate
[PMID: 29975532]
Neutrophil IC50
0.2 μM
Compound: 13
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation preincubated for 5 mins followed by cytochalasin B/fMLP addition for 3 mins by superoxide dismutase inhibitable reduction of ferricytochro
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation preincubated for 5 mins followed by cytochalasin B/fMLP addition for 3 mins by superoxide dismutase inhibitable reduction of ferricytochro
[PMID: 29975532]
Neutrophil IC50
3.5 μM
Compound: 15
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry
Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry
[PMID: 24798144]
SH-SY5Y EC50
> 50 μM
Compound: 33
Neuroprotective activity in human SH-SY5Y cells assessed as reduction in 1-methyl-4-phenylpyridinium ion-induced cell death after 48 hrs by MTT assay
Neuroprotective activity in human SH-SY5Y cells assessed as reduction in 1-methyl-4-phenylpyridinium ion-induced cell death after 48 hrs by MTT assay
[PMID: 27420919]
SH-SY5Y EC50
8.4 μM
Compound: 33
Neuroprotective activity in human SH-SY5Y cells assessed as reduction in oxygen glucose deprivation-induced cell death incubated for 16 hrs under hypoxic condition followed by incubation for 24 hrs under normoxic condition by MTT assay
Neuroprotective activity in human SH-SY5Y cells assessed as reduction in oxygen glucose deprivation-induced cell death incubated for 16 hrs under hypoxic condition followed by incubation for 24 hrs under normoxic condition by MTT assay
[PMID: 27420919]
體外研究
(In Vitro)

Imperatorin 是一種植物次生代謝產(chǎn)物,屬于香豆素類,特別是呋喃香豆素類。Imperatorin 通過 α1β2γ2S 受體增強 GABA 誘導(dǎo)的氯離子電流(IGABA)。Imperatorin 對 IGABA 的增強作用在 100 μmol 時分別為 50.5 %和 300 μmol 時為 109.8 %。Imperatorin 和 Phellopterin,發(fā)現(xiàn)于白芷的根部,在體外抑制 [3H] 地西泮與大鼠腦 GABAA 受體的苯二氮?類位點結(jié)合,Imperatorin 的 IC50 為 12.3 μmol,而 Phellopterin 為 400 nmol。Imperatorin 在 3.5 ~ 14 mmol 濃度范圍內(nèi),通過不可逆地與 GABA-T 活性位點結(jié)合,以時間和濃度依賴性方式顯著地不可逆地抑制 GABA-T。Imperatorin 是一種可逆性乙酰膽堿酯酶(AChE)抑制劑,其作用呈劑量依賴性。采用分光光度法檢測 Imperatorin 和當歸果實粗提物在12.5、25、50、100 μg/mL 濃度下的 AChEBChE 抑制活性。Imperatorin 對 AChE 的抑制率為 13.75 ~ 46.11%,而對BChE的抑制率為37.46 ~ 83.98%。Imperatorin 對 BChE 而非 AChE 具有選擇性,其對 BChE 的 IC50為 31.4 μmol。Imperatorin 和 (+)-Byakangelicol 被發(fā)現(xiàn)是最有效的 BACE-1 抑制劑,其 IC50s 分別為 91.8 和104.9 μmol。Imperatorin(IC50=9.2 μmol)也能有效抑制 NO 合成[1]。
Imperatorin 是 TRPV1 的弱激動劑, TRPV1 參與檢測多種傷害性刺激,表現(xiàn)為EC50為12.6±3.2 μM[2]。

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

體內(nèi)研究
(In Vivo)

Imperatorin (10, 20 mg/kg)注射后30分鐘表現(xiàn)出抗焦慮作用,并改善了記憶和學習過程的不同階段,包括獲得和鞏固[1]。
Imperatorin(10, 20 mg/kg) 可以降低尼古丁(0.1 mg/kg,s.c)的焦慮效應(yīng)[1]。
Imperatorin(30, 40 mg/kg, i.p. )著增強卡馬西平對電休克誘導(dǎo)的最大驚厥的抗驚厥活性,分別將ED50從10.8 mg/kg降至6.8 mg/kg(34%)和6 mg/kg(42%)[1]
Imperatorin(10, 20 mg/kg) 和卡馬西平6.8 mg/kg 使卡馬西平的腦總濃度從1.260 μg/mL增加到2.328 μg/mL(增加了85%),這可能是通過改變血屏障通透性或像多藥耐藥蛋白的抑制劑引起的[1]。
Imperatorin 可使γ -氨基丁酸轉(zhuǎn)氨酶失活并抑制乙酰膽堿酯酶活性[1]。
Imperatorin(5和10 mg/kg)急性給藥可改善東莨菪堿損害的記憶獲取和鞏固, 在注射東莨菪堿(1 mg/kg)之前[1]
Imperatorin (10 mg/kg, 7天,每天2次)顯著減弱東莨菪堿對記憶獲取的影響,而當測定記憶鞏固時,5和10 mg/kg的 Imperatorin 有效[3]

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

分子量

270.28

Formula

C16H14O4

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

歐前胡素;白茅苷;前胡素;主人草素;白芷乙素;歐芹屬素乙;前胡內(nèi)酯

結(jié)構(gòu)分類
初始來源
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 : 50 mg/mL (184.99 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 3.6999 mL 18.4993 mL 36.9987 mL
5 mM 0.7400 mL 3.6999 mL 7.3997 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, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.25 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.25 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

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
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 98.72%

參考文獻
Animal Administration
[3]

Mice[3]
The experiments are carried out on naive male Swiss mice weighing 20-25 g. Drugs are administered intraperitoneally (i.p.) at the volume of 10 mL/kg. Fresh drug solutions are prepared on each day of experimentation. Control groups receive saline injections of the same volume and via the same route of administration. During the acute treatment, the animals are allocated to the following drug groups: saline, rivastigmine (0.5 mg/kg, i.p.), scopolamine (1 mg/kg, i.p.), Imperatorin (1, 5, 10 mg/kg, i.p.), or Imperatorin coadministered with scopolamine. To measure the memory acquisition processes, scopolamine is administered 20 min before the pretest, whereas Imperatorin and rivastigmine are administered 30 min before the pretest. To measure the memory consolidation processes, rivastigmine or scopolamine (1 mg/kg) is administered immediately after the pretest, whereas Imperatorin is administered 15 min after pretest or after scopolamine injection. On the second day, the mice are retested. In the second set of the experiments, animals are randomly allocated to receive 6 days of i.p. injections of Imperatorin (1, 5, and 10 mg/kg, i.p.) or saline, twice daily (8:00 a.m. and 8:00 p.m.). On the seventh day, these animals are subjected to saline, scopolamine (1 mg/kg, i.p.), Imperatorin (1, 5, and 10 mg/kg, i.p.), or Imperatorin coadministered with scopolamine. To measure the memory acquisition processes, scopolamine is administered 20 min before the pretest and Imperatorin 30 min before the pretest. To measure the memory consolidation processes, scopolamine (1 mg/kg) is administered immediately after the pretest, whereas Imperatorin is administered 15 min after the pretest or after scopolamine injection. On the eighth day, the mice are retested.

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(fù)凍融造成的產(chǎn)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(nèi)使用, -20°C儲存時,請在1年內(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 3.6999 mL 18.4993 mL 36.9987 mL 92.4967 mL
5 mM 0.7400 mL 3.6999 mL 7.3997 mL 18.4993 mL
10 mM 0.3700 mL 1.8499 mL 3.6999 mL 9.2497 mL
15 mM 0.2467 mL 1.2333 mL 2.4666 mL 6.1664 mL
20 mM 0.1850 mL 0.9250 mL 1.8499 mL 4.6248 mL
25 mM 0.1480 mL 0.7400 mL 1.4799 mL 3.6999 mL
30 mM 0.1233 mL 0.6166 mL 1.2333 mL 3.0832 mL
40 mM 0.0925 mL 0.4625 mL 0.9250 mL 2.3124 mL
50 mM 0.0740 mL 0.3700 mL 0.7400 mL 1.8499 mL
60 mM 0.0617 mL 0.3083 mL 0.6166 mL 1.5416 mL
80 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
100 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9250 mL
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產(chǎn)品名稱:
Imperatorin
目錄號:
HY-N0285
需求量: