Leelamine (Synonyms: (+)-デヒドロアビエチルアミン)

Name: Leelamine
Brand: MedChemExpress
SKU: HY-W005629
Rating: 4.5 (0 reviews)

製品番号: HY-W005629 純度: 95.69%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Leelamine 構造式

CAS 番号 : 1446-61-3

容量	価格（税別）	在庫状況	数量
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	在庫あり	Estimated Time of Arrival: December 31
Solid or liquid
500 mg	$50	在庫あり	Estimated Time of Arrival: December 31
1 g	$70	在庫あり	Estimated Time of Arrival: December 31
5 g		お問い合わせ
10 g		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Leelamine:

Leelamine hydrochloride 在庫あり

Cannabinoid Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

CB1 CB2

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

CB1

CB2

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	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]
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]
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	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	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	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	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]
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]
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 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]
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]
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	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]
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	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]
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]

体外実験

Leelamine (3 μM, 3 h) induces vacuolization of cells, accumulation of lipofuscin-like material, formation of web-like membrane whorls and inhibition of autophagic flux in melanoma cells^[2].
Leelamine (3 μM, 3 h) induces intracellular cholesterol accumulation and alters cholesterol subcellular localization in UACC 903 or 1205 Lu melanoma cells^[2].
Leelamine (3-5 μM, 3-12 h) inhibits signaling pathways driving melanoma cell survival and disrupts RTK signaling via interference with intracellular vesicular transport systems^[2].

MedChemExpress (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

285.48

分子式

C₂₀H₃₁N

CAS 番号

1446-61-3

Appearance

<44.5°C Solid,>44.5°C Liquid

Color

Colorless to light yellow

SMILES

NC[C@]1(C)CCC[C@]2(C)C3=C(CC[C@@]12[H])C=C(C(C)C)C=C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

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

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (350.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5029 mL	17.5144 mL	35.0287 mL
5 mM	0.7006 mL	3.5029 mL	7.0057 mL
10 mM	0.3503 mL	1.7514 mL	3.5029 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (17.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (17.51 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (17.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 95.79%

Select Batch:

データシート (274 KB) SDS (394 KB)

COA (247 KB) HNMR (123 KB) RP-HPLC (241 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Merarchi M, et, al. A Brief Overview of the Antitumoral Actions of Leelamine. Biomedicines. 2019 Jul 19;7(3):53. [Content Brief]

[2]. Kuzu OF, Gowda R, Sharma A, Robertson GP. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014;13(7):1690-1703. [Content Brief]

[3]. Aicher TD, et al. Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK). Bioorg Med Chem Lett. 1999 Aug 2;9(15):2223-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5029 mL	17.5144 mL	35.0287 mL	87.5718 mL
	5 mM	0.7006 mL	3.5029 mL	7.0057 mL	17.5144 mL
	10 mM	0.3503 mL	1.7514 mL	3.5029 mL	8.7572 mL
	15 mM	0.2335 mL	1.1676 mL	2.3352 mL	5.8381 mL
	20 mM	0.1751 mL	0.8757 mL	1.7514 mL	4.3786 mL
	25 mM	0.1401 mL	0.7006 mL	1.4011 mL	3.5029 mL
	30 mM	0.1168 mL	0.5838 mL	1.1676 mL	2.9191 mL
	40 mM	0.0876 mL	0.4379 mL	0.8757 mL	2.1893 mL
	50 mM	0.0701 mL	0.3503 mL	0.7006 mL	1.7514 mL
	60 mM	0.0584 mL	0.2919 mL	0.5838 mL	1.4595 mL
	80 mM	0.0438 mL	0.2189 mL	0.4379 mL	1.0946 mL
	100 mM	0.0350 mL	0.1751 mL	0.3503 mL	0.8757 mL

Leelamine Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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.

Keywords:

Leelamine1446-61-3PDK-1Environmental PollutantsCannabinoid Receptor3-Phosphoinositide-dependent protein kinase 1Environmental Contaminantsorally activePDKblood glucose loweringdiabetic mousecannabinoid receptorscancer cellsInhibitorinhibitorinhibit

最近チェックした製品:

製品名

カスタマ需要量 *

お名前 *

タイトル

メールアドレス *

電話番号 *

デパートメント

組纖名 *

市区町村

都道府県

国或いは地域 *

必ず会社名を記載ください。個人への返信は行いません。

備考

製品名

Lot #

お名前 *

メールアドレス *

電話番号 *

部門 *

組纖名 *

国或いは地域 *

備考

Leelamine (Synonyms: (+)-デヒドロアビエチルアミン)

カスタマーレビュー

Other Forms of Leelamine:

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Cannabinoid Receptor アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Leelamine Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

お名前
メール *

	Sorry, but the email address you supplied was invalid.

Leelamine (Synonyms: (+)-デヒドロアビエチルアミン)

カスタマーレビュー

Other Forms of Leelamine:

Leelamine 関連抗体

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Cannabinoid Receptor アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Leelamine 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Leelamine Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report