Leelamine (hydrochloride) - CAS:16496-99-4

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Leelamine (hydrochloride) (Synonyms:脱氢松香胺盐酸盐)

目录号 : KCM11875 CAS No. : 16496-99-4 纯度 : ≥98%

Data Sheet SDS 产品使用指南

Leelamine is a diterpene molecule whose name derives from the Sanskrit word leela which means “play”. It has weak affinity for the human central cannabinoid (CB) and peripheral cannabinoid (CB) receptors, exhibiting 20% displacement of [H]-CP55940 at a concentration of 10 µM. Leelamine inhibits pyruvate dehydrogenase kinase (PDK) with an IC of 9.5 µM. Derivatives of leelamine exhibit anti-inflammatory activity and show moderate inhibition of phospholipase A activity from a variety of sources.

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock

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生物活性

Leelamine (hydrochloride) is an orally active weakly basic amine that inhibits NPC1 and the androgen receptor AR-V7, and acts as a cannabinoid receptor agonist. Leelamine hydrochloride also functions as a lysosome affinity agent that blocks endocytosis, disrupts autophagic flux and cholesterol transport, thereby altering the RTK-AKT/STAT/MAPK signaling cascade. Leelamine hydrochloride induces cancer cell death and autophagosome accumulation, and can be used in research related to melanoma, castration-resistant prostate cancer and breast cancer.

体外研究

Leelamine (hydrochloride) (6, 10, 100 μM) can effectively inhibit the proliferation and induce apoptosis of UACC 903 and 1205 Lu metastatic melanoma cells, with corresponding IC₅₀ values of 1.35 μM and 1.93 μM, respectively. Its mechanism of action is to disrupt cholesterol transport and inhibit oncogenic signaling pathways.

Leelamine (hydrochloride) (1, 2, 3, 4, 5 μM) can induce dose-dependent apoptosis in MDA-MB-231, MCF-7, and SUM159 breast cancer cells, without affecting normal MCF-10A breast epithelial cells, and can also inhibit self-renewal of breast cancer stem cells.

Leelamine (hydrochloride) (0.62-100 μmol/L; 72 h) can effectively kill UACC 903 and 1205 Lu melanoma cells, with IC₅₀ values of 1.35 μmol/L and 1.93 μmol/L, respectively; However, its activity against normal FF2441 fibroblasts is weak, with an IC₅₀ of 8.91 μmol/L; Its cytotoxic activity can be reversed by bafilomycin A1 or β - cyclodextrin.

Leelamine (hydrochloride) (3, 5, 10 µmol/L; 24 hours) can induce non caspase dependent cell death in UACC 903 and 1205 Lu melanoma cells at concentrations as low as 3 µmol/L, which partially relies on autophagy flow; HCT116 cells with BAX gene knockout showed enhanced resistance to it, while the cell death activity of normal fibroblasts decreased at this concentration; Vacuole H⁺- ATPase inhibitors or consumption of cholesterol through β - cyclodextrin can prevent this type of cell death.

Leelamine (hydrochloride) (3.0-5.0 μmol/L; 24 h) can dose dependently inhibit autophagic flow in UACC 903 melanoma cells, which can be confirmed by the increase in p62 and LC3B protein levels after treatment with 3.0, 4.0, and 5.0 μmol/L for 24 hours.

Leelamine (hydrochloride) (3.0-5.0 μmol/L; 24 hours) can inhibit the PI3K/AKT, STAT3, and MAPK oncogenic signaling pathways in UACC 903 melanoma cells after treatment at concentrations of 3.0, 4.0, and 5.0 μmol/L for 24 hours.
Leelamine (3 µmol/L; 30-45 min) acts as a lysosome targeting compound in UACC 903 melanoma cells, with an uptake rate of 60% within 30 minutes. At a concentration of 3 µmol/L, it reduces the uptake of LysoTracker Red DND-99 and its vacuolization activity can be inhibited by vacuolar H⁺- ATPase inhibitors.

体内研究

Leelamine (hydrochloride) (80 mg/kg, administered orally) can reduce the volume of melanoma xenografts in nude mice by 50% and inhibit tumor proliferation without significant systemic toxicity
Leelamine (hydrochloride) (7.5 mg/kg; intraperitoneal injection; 5 times a week) can inhibit the growth of in situ SUM159 breast cancer xenograft in female nude mice by 70%, and there is no obvious systemic toxicity.
Leelamine (hydrochloride) (80 mg/kg; oral; Daily; 3-4 weeks) can inhibit the tumor growth of xenograft melanoma in female thymus free nu/nu mice, with extremely low systemic toxicity.

Animal Model:	Nude mice (female)
Dosage:	7.5 mg/kg
Administration:	i.p.; 5 times per week
Result:	Suppressed tumor growth by 70%. Showed no significant systemic toxicity after treatment. Caused no changes in body weight, blood parameters, or organ morphology after treatment.

Animal Model:	athymic nu/nu (female, 4-6 weeks old)
Dosage:	80 mg/kg
Administration:	p.o.; daily; 3-4 weeks
Result:	Reduced tumor volume by an amount comparable to the 51% reduction seen with analog compound 4a. Showed no significant differences in body weights compared to vehicle controls. Resulted in blood biomarkers of organ toxicity (ALT, AST, ALKP, ALB, GLB, TPR, TBIL, BUN, GLU, CK, CAL) falling within the normal range for this mouse species.

分子式

C₂₀H₃₁N^.HCl

分子量

321.93

CAS号

16496-99-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

溶解性数据

In Vitro:

DMSO : 25 mg/mL (77.66 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

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

此方案可获得 ≥ 2.5 mg/mL (7.77 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

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

此方案可获得 ≥ 2.5 mg/mL (7.77 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

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

此方案可获得 ≥ 2.5 mg/mL (7.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。