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1-Monopalmitin

Cat No.:V45722 Purity: ≥98%
1-Monopalmitin is a bitter melon extract that can inhibit P-glycoprotein (P-gp) activity in intestinal Caco-2 cells.
1-Monopalmitin
1-Monopalmitin Chemical Structure CAS No.: 542-44-9
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
1-Monopalmitin is a bitter melon extract that can inhibit P-glycoprotein (P-gp) activity in intestinal Caco-2 cells.
1-Monopalmitin (Glyceryl palmitate) is a small molecule compound extracted from Mougeotia nummuloides and Spirulina major, as well as from bitter melon. It has demonstrated potential antitumor activity and functions as a P-glycoprotein (P-gp) inhibitor. 1-Monopalmitin induces protective autophagy and apoptosis in lung cancer cells while exhibiting low toxicity to normal cells. It is primarily used in research applications studying cancer biology, drug resistance mechanisms, and P-gp-mediated drug transport.
Biological Activity I Assay Protocols (From Reference)
Targets
1-Monopalmitin targets P-glycoprotein (P-gp), an efflux transporter involved in multidrug resistance. It inhibits P-gp activity in intestinal Caco-2 cells, thereby increasing drug accumulation. The compound also modulates the PI3K/Akt signaling pathway. By inhibiting P-gp, 1-Monopalmitin can reverse multidrug resistance and enhance the intracellular concentration of chemotherapeutic agents that are P-gp substrates.
ln Vitro
1-Monopalmitin significantly inhibits the proliferation of A549 and SPC-A1 lung cancer cells in vitro, with IC₅₀ values of 50-58 µg/mL. It induces G2/M cell cycle arrest and caspase-dependent apoptosis. The compound also inhibits P-gp activity in intestinal Caco-2 cells, leading to increased intracellular accumulation of P-gp substrates. It induces protective autophagy alongside apoptosis in cancer cells.
ln Vivo
In vivo activity data for 1-Monopalmitin are limited in the available literature. Based on its in vitro antitumor activity against lung cancer cell lines and its P-gp inhibitory properties, it is anticipated to have potential in vivo efficacy in tumor models when used alone or in combination with chemotherapeutic agents. However, specific in vivo studies detailing its pharmacokinetics and efficacy in animal models are not extensively documented.
Enzyme Assay
The non-cellular enzyme/receptor binding assay for 1-Monopalmitin typically involves P-gp ATPase activity assays using membrane preparations from cells overexpressing human P-gp. The compound's ability to stimulate or inhibit P-gp ATPase activity is measured by quantifying inorganic phosphate released from ATP hydrolysis. Alternatively, vesicular transport assays using inside-out membrane vesicles can measure the uptake of radiolabeled P-gp substrates in the presence of 1-Monopalmitin.
Cell Assay
In vitro cellular assays for 1-Monopalmitin commonly use human lung cancer cell lines such as A549 and SPC-A1. Cells are treated with various concentrations of the compound for 24-72 hours. Cell proliferation is assessed using MTT or CCK-8 assays. Cell cycle distribution is analyzed by flow cytometry with propidium iodide staining. Apoptosis is detected by Annexin V/PI staining and caspase activity assays. P-gp activity is evaluated in Caco-2 cells using fluorescent substrates such as rhodamine 123.
Animal Protocol
In vivo animal studies for 1-Monopalmitin are not well documented in the available literature. Based on its mechanism as a P-gp inhibitor and antitumor agent, typical study designs would involve xenograft mouse models bearing human lung cancer tumors. 1-Monopalmitin would be administered orally or intraperitoneally, either alone or in combination with chemotherapeutic drugs like paclitaxel or doxorubicin. Tumor volume, body weight, and survival rates would be monitored.
ADME/Pharmacokinetics
Pharmacokinetic properties of 1-Monopalmitin are not extensively characterized in the literature. As a monoglyceride, it is expected to be absorbed through intestinal lymphatic pathways. Its inhibition of P-gp in intestinal Caco-2 cells suggests that it may affect the oral bioavailability of co-administered P-gp substrates. The compound is likely metabolized by lipases and esterases to palmitic acid and glycerol. Specific parameters such as half-life, Cmax, and bioavailability are not well documented.
Toxicity/Toxicokinetics
Toxicological data for 1-Monopalmitin indicate low toxicity to normal cells, as it has been shown to induce apoptosis preferentially in cancer cells while sparing normal cells. The compound is generally recognized as safe for research applications. However, comprehensive toxicology studies including acute and chronic toxicity, genotoxicity, and organ-specific toxicity are not extensively available in the literature.
References

[1]. A bitter melon extract inhibits the P-glycoprotein activity in intestinal Caco-2 cells: monoglyceride as an active compound. Biofactors. 2004;22(1-4):71-4.

Additional Infomation
1-Monopalmitoylglycerol is a 1-monoglyceride with a palmitoyl group. It is a natural product discovered in Neolitsea daibuensis. It is a metabolite found in both plants and algae. Its function is related to hexadecanoic acid. Palmitoylglycerol has been reported in Perilla frutescens, Trichosanthes tricuspidata, and other organisms with relevant data. See also: Glycerides, C16-22 (note moved to); Palmitoylglycerol (note moved to).
1-Monopalmitin is a research-grade compound not approved for clinical use. Its primary research applications include studying P-gp-mediated multidrug resistance, investigating anticancer mechanisms involving autophagy and apoptosis, and exploring PI3K/Akt signaling modulation. The compound is also known as Glyceryl palmitate and is used as a reference standard in analytical studies. It is intended for laboratory research use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H38O4
Molecular Weight
330.5026
Exact Mass
330.277
CAS #
542-44-9
PubChem CID
14900
Appearance
White to off-white solid powder
Density
0.969g/cm3
Boiling Point
451.3ºC at 760mmHg
Melting Point
75ºC
Flash Point
146.7ºC
LogP
4.364
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
18
Heavy Atom Count
23
Complexity
256
Defined Atom Stereocenter Count
0
InChi Key
QHZLMUACJMDIAE-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H38O4/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-19(22)23-17-18(21)16-20/h18,20-21H,2-17H2,1H3
Chemical Name
2,3-dihydroxypropyl hexadecanoate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
Ethanol : ~50 mg/mL (~151.28 mM)
DMSO : ~50 mg/mL (~151.28 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0257 mL 15.1286 mL 30.2572 mL
5 mM 0.6051 mL 3.0257 mL 6.0514 mL
10 mM 0.3026 mL 1.5129 mL 3.0257 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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