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  2. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR
  3. Cannabinoid Receptor PDK-1
  4. Leelamine

Leelamine  (Synonyms: 脫氫松香胺)

目錄號(hào): HY-W005629 純度: ≥98.0%
COA 產(chǎn)品使用指南

Leelamine 是具有口服活性的丙酮酸脫氫酶激酶 (PDK) 抑制劑，IC50 值為 9.5 μM，在糖尿病小鼠中表現(xiàn)出降血糖效果。Leelamine 也是 CB1 和 CB2 大麻素受體的弱激動(dòng)劑。Leelamine 降低癌細(xì)胞有絲分裂活性、前列腺特異性抗原表達(dá)，并誘導(dǎo)癌細(xì)胞凋亡 (Apoptosis)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Leelamine Chemical Structure

Leelamine Chemical Structure

CAS No. : 1446-61-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥220
In-stock
500 mg ￥200
In-stock
1 g ￥300
In-stock
5 g   詢(xún)價(jià)  
10 g   詢(xún)價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Leelamine:

查看 Cannabinoid Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells[1][2][3].

IC50 & Target[1]

CB1

 

CB2

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
5637 IC50
8.7 μM
Compound: 3
Cytotoxicity against human 5637 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human 5637 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23707051]
A2780 EC50
3.8 μM
Compound: Dehydroabietylamine
Cytotoxicity against human A2780 cells after 96 hrs by sulforhodamine-B assay
Cytotoxicity against human A2780 cells after 96 hrs by sulforhodamine-B assay
[PMID: 30056282]
A549 IC50
5.02 μM
Compound: L0
Antineoplastic activity against human A549 cells measured after 36 hrs by MTT assay
Antineoplastic activity against human A549 cells measured after 36 hrs by MTT assay
[PMID: 30746067]
A549 IC50
5.02 μM
Compound: L0
Antiproliferative activity against human A549 cells after 36 hrs by MTT assay
Antiproliferative activity against human A549 cells after 36 hrs by MTT assay
[PMID: 29407970]
EJ IC50
4.82 μM
Compound: 3
Cytotoxicity against human EJ cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human EJ cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23707051]
FaDu EC50
3.9 μM
Compound: Dehydroabietylamine
Cytotoxicity against human FADU cells after 96 hrs by sulforhodamine-B assay
Cytotoxicity against human FADU cells after 96 hrs by sulforhodamine-B assay
[PMID: 30056282]
HeLa IC50
2.02 μM
Compound: L0
Antineoplastic activity against human HeLa cells measured after 36 hrs by MTT assay
Antineoplastic activity against human HeLa cells measured after 36 hrs by MTT assay
[PMID: 30746067]
HeLa IC50
2.02 μM
Compound: L0
Antiproliferative activity against human HeLa cells after 36 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 36 hrs by MTT assay
[PMID: 29407970]
HeLa IC50
7.68 μM
Compound: 3
Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23707051]
HepG2 IC50
2.56 μM
Compound: L0
Antineoplastic activity against human HepG2 cells measured after 36 hrs by MTT assay
Antineoplastic activity against human HepG2 cells measured after 36 hrs by MTT assay
[PMID: 30746067]
HepG2 IC50
2.56 μM
Compound: L0
Antiproliferative activity against human HepG2 cells after 36 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 36 hrs by MTT assay
[PMID: 29407970]
HT-29 EC50
2.1 μM
Compound: Dehydroabietylamine
Cytotoxicity against human HT-29 cells after 96 hrs by sulforhodamine-B assay
Cytotoxicity against human HT-29 cells after 96 hrs by sulforhodamine-B assay
[PMID: 30056282]
HUVEC IC50
1.27 μM
Compound: L0
Cytotoxicity against HUVEC measured after 36 hrs by MTT assay
Cytotoxicity against HUVEC measured after 36 hrs by MTT assay
[PMID: 30746067]
HUVEC IC50
1.27 μM
Compound: L0
Cytotoxicity against HUVEC assessed as reduction in cell viability after 36 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability after 36 hrs by MTT assay
[PMID: 29407970]
J774 CC50
14.5 μM
Compound: 6
Cytotoxicity against mouse J774 cells assessed as reduction of cell viability after 48 hrs by resazurin dye-based fluorometric method
Cytotoxicity against mouse J774 cells assessed as reduction of cell viability after 48 hrs by resazurin dye-based fluorometric method
[PMID: 27318121]
Jurkat IC50
4.85 μM
Compound: 3
Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23707051]
L6 IC50
6.5 μM
Compound: 1; TCI D1588
Cytotoxicity against rat L6 cells after 72 hrs by AlamarBlue dye based fluorimetric method
Cytotoxicity against rat L6 cells after 72 hrs by AlamarBlue dye based fluorimetric method
[PMID: 26849852]
L6 IC50
7.4 μM
Compound: 1; TCI D1588
Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by photometric method
Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by photometric method
[PMID: 26849852]
MCF7 IC50
19.45 μM
Compound: L0
Antineoplastic activity against human MCF7 cells measured after 36 hrs by MTT assay
Antineoplastic activity against human MCF7 cells measured after 36 hrs by MTT assay
[PMID: 30746067]
MCF7 IC50
19.45 μM
Compound: L0
Antiproliferative activity against human MCF7 cells after 36 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 36 hrs by MTT assay
[PMID: 29407970]
MCF7 EC50
3 μM
Compound: Dehydroabietylamine
Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine-B assay
Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine-B assay
[PMID: 30056282]
NIH3T3 EC50
2.4 μM
Compound: Dehydroabietylamine
Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by sulforhodamine-B assay
Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by sulforhodamine-B assay
[PMID: 30056282]
PC-3 IC50
7.88 μM
Compound: 3
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23707051]
SW-1736 EC50
4.2 μM
Compound: Dehydroabietylamine
Cytotoxicity against human SW1736 cells after 96 hrs by sulforhodamine-B assay
Cytotoxicity against human SW1736 cells after 96 hrs by sulforhodamine-B assay
[PMID: 30056282]
體外研究
(In Vitro)

Leelamine (3 μM, 3 小時(shí)) 誘導(dǎo)黑色素瘤細(xì)胞的細(xì)胞空泡化，類(lèi)脂褐素物質(zhì)的積累，形成網(wǎng)狀膜渦卷，并抑制自噬流動(dòng)[2]。
Leelamine (3 μM, 3 小時(shí)) 誘導(dǎo) UACC 903 或 1205 Lu 黑色素瘤細(xì)胞內(nèi)膽固醇積累，并改變膽固醇的亞細(xì)胞定位[2]。
Leelamine (3-5 μM, 3-12 小時(shí)) 抑制驅(qū)動(dòng)黑色素瘤細(xì)胞生存的信號(hào)通路，并通過(guò)干擾細(xì)胞內(nèi)囊泡運(yùn)輸系統(tǒng)來(lái)破壞 RTK 信號(hào)傳導(dǎo)[2]。

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

Western Blot Analysis[2]

Cell Line: Melanoma cells
Concentration: 3-5 μM
Incubation Time: 3-12 h
Result: Significantly decreased phosphorylation of EIF4EBP1 (4E-BP1) and inhibited AKT/mTOR branch of the cascade in melanoma cells.

Immunofluorescence[2]

Cell Line: UACC 903 melanoma cells
Concentration: 3 μM
Incubation Time: 3 h
Result: Induced vacuolization of UACC 903 melanoma cells and autophagosome accumulation, followed by membrane blebbing, cell shrinkage and cell rounding.
分子量

285.47

Formula

C20H31N
CAS 號(hào)
性狀

<44.5°C 固體,>44.5°C 液體

顏色

Colorless to light yellow

運(yùn)輸條件

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (350.30 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 3.5030 mL 17.5150 mL 35.0299 mL
5 mM 0.7006 mL 3.5030 mL 7.0060 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 (protect from light)。-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)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.76 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。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.76 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
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
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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: 98.36%

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 (protect from light)。-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 3.5030 mL 17.5150 mL 35.0300 mL 87.5749 mL
5 mM 0.7006 mL 3.5030 mL 7.0060 mL 17.5150 mL
10 mM 0.3503 mL 1.7515 mL 3.5030 mL 8.7575 mL
15 mM 0.2335 mL 1.1677 mL 2.3353 mL 5.8383 mL
20 mM 0.1751 mL 0.8757 mL 1.7515 mL 4.3787 mL
25 mM 0.1401 mL 0.7006 mL 1.4012 mL 3.5030 mL
30 mM 0.1168 mL 0.5838 mL 1.1677 mL 2.9192 mL
40 mM 0.0876 mL 0.4379 mL 0.8757 mL 2.1894 mL
50 mM 0.0701 mL 0.3503 mL 0.7006 mL 1.7515 mL
60 mM 0.0584 mL 0.2919 mL 0.5838 mL 1.4596 mL
80 mM 0.0438 mL 0.2189 mL 0.4379 mL 1.0947 mL
100 mM 0.0350 mL 0.1751 mL 0.3503 mL 0.8757 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)：
Leelamine
目錄號(hào)：
HY-W005629
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