Leelamine hydrochloride

Name: Leelamine hydrochloride
Brand: MedChemExpress
SKU: HY-110028
Rating: 4.5 (1 reviews)

Cat. No.: HY-110028 Purity: 99.06%: FAQs
Data Sheet SDS COA Handling Instructions

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Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis^[2,3].

For research use only. We do not sell to patients.

Leelamine hydrochloride Chemical Structure

CAS No. : 16496-99-4

Size	Price	Stock	Quantity
5 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Leelamine hydrochloride:

Leelamine Get quote

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CB1 CB2

Biological Activity
Purity & Documentation
References
Customer Review

Description

Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees^[1]. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. Leelamine hydrochloride suppresses transcriptional activity of androgen receptor, which is known to regulate fatty acid synthesis^[2,3].

IC₅₀ & Target^[2]

CB1

Molecular Weight

321.93

Formula

C₂₀H₃₂ClN

CAS No.

16496-99-4

Appearance

Solid

Color

White to off-white

SMILES

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

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (77.66 mM; ultrasonic and warming and heat to 60°C; 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	3.1063 mL	15.5313 mL	31.0627 mL
5 mM	0.6213 mL	3.1063 mL	6.2125 mL
10 mM	0.3106 mL	1.5531 mL	3.1063 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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: ≥ 2.5 mg/mL (7.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (sealed storage, away from moisture)

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.

Purity & Documentation

Purity: 99.06%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (248 KB) HNMR (158 KB) RP-HPLC (204 KB) LCMS (235 KB)

Handling Instructions (2659 KB)

References

[1]. Kuzu OF, et al. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014 Jul;13(7):1690-703. [Content Brief]

[2]. A.O. Ibegbu, et al. Therapeutic Potentials and uses of Cannabinoid Agonists in Health and Disease Conditions. British Journal of Pharmacology and Toxicology 3(2): 76-88, 2012

[3]. Singh KB, et al. Leelamine is a Novel Lipogenesis Inhibitor in Prostate Cancer Cells In Vitro and In Vivo. Mol Cancer Ther. 2019 Aug 8. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.1063 mL	15.5313 mL	31.0627 mL	77.6566 mL
	5 mM	0.6213 mL	3.1063 mL	6.2125 mL	15.5313 mL
	10 mM	0.3106 mL	1.5531 mL	3.1063 mL	7.7657 mL
	15 mM	0.2071 mL	1.0354 mL	2.0708 mL	5.1771 mL
	20 mM	0.1553 mL	0.7766 mL	1.5531 mL	3.8828 mL
	25 mM	0.1243 mL	0.6213 mL	1.2425 mL	3.1063 mL
	30 mM	0.1035 mL	0.5177 mL	1.0354 mL	2.5886 mL
	40 mM	0.0777 mL	0.3883 mL	0.7766 mL	1.9414 mL
	50 mM	0.0621 mL	0.3106 mL	0.6213 mL	1.5531 mL
	60 mM	0.0518 mL	0.2589 mL	0.5177 mL	1.2943 mL