| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
IC50: antiangiogenic
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|---|---|
| ln Vitro |
Morel acid, at a low concentration of 0.5 µM, can inhibit HUVEC migration in in vitro experiments on HUVEC cell migration [1].
- Morellic acid exhibited cytotoxicity against four human cancer cell lines (HeLa, A549, HCT-116, HepG-2) and inhibited proliferation of HUVEC cells in MTT assays. The IC50 values were: HeLa 13.78 μM, A549 14.23 μM, HCT-116 8.89 μM, HepG-2 13.34 μM, and HUVEC 6.14 μM. [2] - Morellic acid at a concentration of 0.5 μM strongly inhibited the migration of HUVEC in a wound migration assay. After wounding, HUVECs were incubated with fresh medium containing 0.5 μM of the compound, and cell movement into the wound area was examined after 24 hours, showing remarkable inhibition compared to control. [2] |
| ln Vivo |
- In a transgenic zebrafish (Tg(flk1:EGFP)) model, Morellic acid showed antiangiogenic activity. At concentrations of 4 μM, 8 μM, 16 μM and 32 μM, it exhibited inhibitory effects on the growth of intersegmental vessels (ISVs). Compared to the water-treated control, most ISVs were incompletely formed. The antiangiogenic effect was comparable to gambogic acid (xanthone 1) but required higher concentrations (active at 4 μM vs. 1-2 μM for gambogic acid). [2]
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| Cell Assay |
- Cytotoxicity and anti-proliferation were assessed by the MTT assay. Human cancer cell lines (HeLa, A549, HCT-116, HepG-2) and HUVEC cells were seeded in 96-well plates and treated with various concentrations of Morellic acid for a specified duration. After treatment, MTT solution was added and incubated for 4 hours, then the formazan crystals were dissolved in DMSO, and absorbance was measured at 570 nm (or reference wavelength). The IC50 values were calculated from dose-response curves. [2]
- HUVEC wound migration assay: HUVECs were seeded at a density of 2×10^5 per well in 6-well plates pre-coated with 1% gelatin and grown overnight in DMEM with 10% FBS until 100% confluence. A wound area was created by scraping the cell monolayer with a plastic tip. Cells were then incubated with fresh DMEM medium containing 0.5 μM Morellic acid. After 24 hours, migration and cell movement into the wound area were examined and photographed. [2] |
| Animal Protocol |
- Antiangiogenic activity assay in zebrafish embryos: A transgenic zebrafish line Tg(flk1:EGFP) was used. Adult zebrafish were maintained at 28.5°C. Embryos were generated by natural pair-wise mating, collected, and raised at 28.5°C in embryo water. At 6 hours post-fertilization (hpf), embryos at the shield stage were sorted and placed into 24-well plates (8 embryos per well) containing 1 mL embryo water. Morellic acid was added at various concentrations (e.g., 1, 2, 4, 8, 16, 32 μM) from the shield stage (about 6 hpf). After 24 hours of drug treatment, embryos were anesthetized with 0.05% 2-phenoxyethanol in embryo water. Then embryos were placed on a slide and examined for the presence of ectopic vessels in the subintestinal vessel plexus (SIV) under a fluorescence microscope. Photographs were taken to assess antiangiogenic effects. [2]
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| Toxicity/Toxicokinetics |
- In zebrafish embryos, Morellic acid caused death of all embryos at the highest concentration tested (8 μM). Death rates: at 1 μM: 0/8; 2 μM: 0/8; 4 μM: 0/8; 8 μM: 8/8 (all dead). [2]
- Morellic acid decreased the heart rates of zebrafish embryos in a concentration-dependent manner. Heart rates (per 10 seconds) were: control (embryo water) 21; at 1 μM: 16; at 2 μM: 10; at 4 μM: 8; at 8 μM: 6; at higher concentrations (16, 32 μM) no data due to death or inactivity. [2] |
| References |
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| Additional Infomation |
(-)-Morellic Acid has been reported in Garcinia gaudichaudii, Garcinia lateriflora, and other organisms with available data.
- Morellic acid (xanthone 3) was isolated from the resin of Garcinia hanburyi along with ten other known caged polyprenylated xanthones (1-11). Its structure was identified by MS, NMR, and UV spectroscopy, and confirmed by comparison with literature data. [2] - The antiangiogenic activity of Morellic acid was evaluated together with gambogic acid (GA), isogambogenic acid, and gambogenin. While GA showed antiangiogenic effects at lower concentrations (1-2 μM), Morellic acid required higher concentrations (≥4 μM) and exhibited greater toxicity (lethal at 8 μM) compared to gambogenin (xanthone 7), which had no toxicity up to 32 μM. [2] |
| Molecular Formula |
C33H36O8
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|---|---|
| Molecular Weight |
560.6342
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| Exact Mass |
453.242
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| CAS # |
5304-71-2
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| PubChem CID |
54580250
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| Appearance |
Orange to red solid
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| Density |
1.36±0.1 g/cm3(Predicted)
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| Boiling Point |
777.6±60.0 °C(Predicted)
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| Melting Point |
94 °C
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| LogP |
4.85
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
41
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| Complexity |
1330
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1C(C([H])([H])[H])(C([H])([H])[H])[C@@]2([H])C([H])([H])[C@]3([H])C([H])=C4C(C5C(=C6C([H])=C([H])C(C([H])([H])[H])(C([H])([H])[H])OC6=C(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])C=5O[C@]24[C@@]1(C([H])([H])/C(/[H])=C(\C(=O)O[H])/C([H])([H])[H])C3=O)O[H])=O
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| InChi Key |
COVMVPHACFXMAX-OYNOKLRGSA-N
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| InChi Code |
InChI=1S/C33H36O8/c1-16(2)8-9-20-26-19(11-12-30(4,5)39-26)24(34)23-25(35)21-14-18-15-22-31(6,7)41-32(28(18)36,13-10-17(3)29(37)38)33(21,22)40-27(20)23/h8,10-12,14,18,22,34H,9,13,15H2,1-7H3,(H,37,38)/b17-10-/t18-,22+,32+,33-/m1/s1
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| Chemical Name |
(Z)-4-[(1S,2S,17S,19R)-12-hydroxy-8,8,21,21-tetramethyl-5-(3-methylbut-2-enyl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoic acid
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~178.37 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 | 1.7837 mL | 8.9185 mL | 17.8371 mL | |
| 5 mM | 0.3567 mL | 1.7837 mL | 3.5674 mL | |
| 10 mM | 0.1784 mL | 0.8919 mL | 1.7837 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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