| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Protein tyrosine phosphatase 1B (PTP1B).
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|---|---|
| ln Vitro |
In vitro, momordicoside A inhibits PTP1B activity, an enzyme that negatively regulates insulin signaling. By inhibiting PTP1B, the compound enhances insulin sensitivity and improves glucose metabolism. It modulates glucose metabolism and suppresses tumor cell proliferation through regulation of pathways such as AMPK and NF-kappaB. The compound also shows anti-inflammatory activity by suppressing pro-inflammatory cytokines and reducing oxidative stress. Analytical methods using SPE-HPLC have been established for the determination of momordicoside A with a linear range of 10-1,000 mg/L (r2 = 0.9992).
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| ln Vivo |
In vivo, momordicoside A has been studied for potential therapeutic roles in managing diabetes, obesity, and cancer. It modulates glucose metabolism and enhances insulin sensitivity. The compound is derived from bitter melon, a traditional medicinal plant used for blood glucose regulation. Detailed in vivo pharmacokinetic and pharmacodynamic data are limited, as the compound is primarily a research-grade natural product.
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| Enzyme Assay |
PTP1B inhibition assays are performed using recombinant human PTP1B enzyme. The assay buffer contains 50 mM citrate (pH 6.0), 100 mM NaCl, 1 mM EDTA, and 1 mM DTT. The substrate (p-nitrophenyl phosphate, pNPP) at 10 mM is added to the enzyme in the presence or absence of momordicoside A at varying concentrations (0.1-100 microM). The reaction is initiated by substrate addition, incubated at 37degC for 30 minutes, and terminated by adding 1 M NaOH. Absorbance is measured at 405 nm. Enzyme activity is calculated based on p-nitrophenol production. IC₅0 values are determined from dose-response curves. For HPLC analysis, samples are processed by solid phase extraction (SPE) on carboplatin cartridges (3 mL/250 mg) and analyzed on a C18 column (4.6 mm × 250 mm, 5 microm) with mobile phase acetonitrile:50 mM KH2PO4 (25:20:60) at 0.8 mL/min with UV detection.
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| Cell Assay |
Cellular assays are performed using insulin-sensitive cell lines such as 3T3-L1 adipocytes or HepG2 hepatocytes. Cells are cultured in appropriate medium and treated with momordicoside A at concentrations ranging from 1-100 microM for 24-48 hours. Insulin-stimulated glucose uptake is measured using 2-deoxy-D-[3H]-glucose or fluorescent glucose analogs. PTP1B activity in cell lysates is measured using phosphatase assay kits. AMPK phosphorylation is assessed by Western blot. Cell viability is evaluated using MTT assays. For anti-proliferative studies, cancer cell lines (e.g., A549, HeLa, MCF-7) are treated with the compound and cell growth is measured by MTT or colony formation assays. Apoptosis is assessed by flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
C57BL/6 or db/db diabetic mice are used to evaluate the anti-diabetic effects of momordicoside A. The compound is administered orally or intraperitoneally at doses ranging from 10-100 mg/kg daily for 2-4 weeks. Fasting blood glucose, oral glucose tolerance test (OGTT), and insulin tolerance test (ITT) are performed. HbA1c levels, serum insulin, and lipid profiles are measured. Tissue samples (liver, adipose) are collected for histological and biochemical analysis (e.g., PTP1B activity, AMPK phosphorylation, inflammatory markers). For anti-tumor studies, xenograft mouse models are used; tumor volume and weight are measured over time.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for momordicoside A are limited. As a triterpenoid saponin (C42H₇2O1₅, MW 817.01), the compound has high molecular weight and multiple glycosyl groups, which may limit oral bioavailability. The compound is soluble in DMSO and other organic solvents. Metabolism likely involves deglycosylation in the gastrointestinal tract, with the aglycone being absorbed. Detailed pharmacokinetic parameters (Tmax, Cmax, half-life) are not reported in the available literature.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for momordicoside A. As a natural product derived from a food plant (bitter melon), it is presumed to have a relatively favorable safety profile. However, high doses or prolonged use may have effects that have not been systematically evaluated. The compound is for research use only and not for human consumption. Standard safety precautions should be observed when handling.
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| References | |
| Additional Infomation |
Momordicoside A is a steroidal saponin, a 3-hydroxysteroid, and a disaccharide derivative. It has been reported that bitter melon contains Momordicoside A, and relevant data is available for reference.
Momordicoside A is a natural product research compound with molecular formula C42H₇2O1₅ and molecular weight 817.01. It is isolated from Momordica charantia L. (bitter melon), a plant traditionally used in various cultures for its medicinal properties. The compound's primary research application is as a PTP1B inhibitor for studying insulin signaling and diabetes pathophysiology. It also has potential applications in cancer research due to its anti-proliferative activity. Momordicoside A is not an approved therapeutic agent and is available for research purposes only as a high-purity natural product standard. |
| Molecular Formula |
C42H72O15
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|---|---|
| Molecular Weight |
817.0121
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| Exact Mass |
816.487
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| CAS # |
75801-95-5
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| PubChem CID |
71717038
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
969.3±65.0 °C at 760 mmHg
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| Flash Point |
540.0±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.610
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| LogP |
3.09
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
57
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| Complexity |
1440
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| Defined Atom Stereocenter Count |
21
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| SMILES |
C[C@@H]([C@H]1CC[C@@]2([C@@]1(CC[C@@]3([C@H]2CC=C4[C@H]3CC[C@@H](C4(C)C)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O)O)O)O)C)C)C)[C@@H]([C@H]([C@H](C(C)(C)O)O)O)O
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| InChi Key |
WBYJYPOPDKQBQJ-WVMSUIAMSA-N
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| InChi Code |
InChI=1S/C42H72O15/c1-19(27(44)32(49)35(52)39(4,5)53)20-13-14-42(8)25-11-9-21-22(40(25,6)15-16-41(20,42)7)10-12-26(38(21,2)3)57-37-34(51)31(48)29(46)24(56-37)18-54-36-33(50)30(47)28(45)23(17-43)55-36/h9,19-20,22-37,43-53H,10-18H2,1-8H3/t19-,20+,22+,23+,24+,25+,26-,27-,28+,29+,30-,31-,32+,33+,34+,35+,36+,37-,40-,41+,42-/m0/s1
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| Chemical Name |
(3R,4R,5S,6S)-2-methyl-6-[(3S,8R,9R,10S,13R,14S,17R)-4,4,9,13,14-pentamethyl-3-[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxy-2,3,7,8,10,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-17-yl]heptane-2,3,4,5-tetrol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~122.40 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2240 mL | 6.1199 mL | 12.2398 mL | |
| 5 mM | 0.2448 mL | 1.2240 mL | 2.4480 mL | |
| 10 mM | 0.1224 mL | 0.6120 mL | 1.2240 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.
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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