| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
NMDA Receptor
Crocetin meglumine targets the NMDA receptor, where it acts as a high-affinity antagonist. It is thought to be responsible for the CNS activity of saffron extract. The compound is capable of crossing the blood-brain barrier (BBB) and reaching the central nervous system. |
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| ln Vitro |
The saffron metabolite crocetin (Transcrocetin) meglumine, which comes from the crocin apocarotenoids, has been demonstrated to have a significant affinity for NMDA receptors and is assumed to be the cause of saffron's central nervous system activity.After a 24-hour incubation period with the test compounds, the cellular mitochondrial dehydrogenase activity of Caco-2 cells is measured by the MTT assay to ensure that the viability of the cells remains unchanged throughout the transport experiments. The results show that neither hydroalcoholic saffron extract (SE, 0.5-1 mg/mL) nor crocin-1 (250-1000 µM) significantly alter the viability of the cells. Cell viability is not affected by crocetin meglumine at 10 µM doses, but it is dramatically reduced at higher concentrations (40–160 µM)[1].
In vitro, Crocetin (Transcrocetin) meglumine exerts strong NMDA receptor affinity and is considered the primary cause of saffron's CNS activity. It has been studied for its neuroprotective effects and ability to modulate glutamatergic signaling in primary neuronal cultures. |
| ln Vivo |
In vivo, crocetin has been studied in preclinical models of Alzheimer's disease. Pharmacokinetic parameters of crocetin have been evaluated after oral administration, both alone and in combination with anti-Alzheimer drugs such as galantamine, donepezil, memantine, and rivastigmine. It shows potential for cognitive enhancement.
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| Enzyme Assay |
Crocetin meglumine is evaluated using standard radioligand binding assays to measure NMDA receptor affinity. Membranes from rat forebrain expressing NMDA receptors are incubated with [3H]MK-801 (dizocilpine) and varying concentrations (0-100 microM) of crocetin meglumine. Non-specific binding is defined using 10 microM unlabeled MK-801. Bound radioactivity is measured by filtration.
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| Cell Assay |
For in vitro cellular assays, primary rat cortical neurons or SH-SY5Y cells are plated in 96-well plates. Cells are treated with crocetin meglumine (0-100 microM) for 24-48 hours. Neuroprotective effects are assessed by challenging with 100 microM NMDA or 50 microM glutamate for 15-30 minutes. Cell viability is measured using MTT or LDH release assay.
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| Animal Protocol |
For in vivo studies, male C57BL/6 mice or Sprague-Dawley rats (6-8 weeks old) are used. Crocetin or crocetin meglumine is administered via oral gavage (e.g., 10-50 mg/kg) or intraperitoneal injection. For PK studies, blood is collected at various time points (0-24 hours). For efficacy studies, cognitive tests (Morris water maze, Y-maze) are performed after chronic dosing for 14-28 days.
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| ADME/Pharmacokinetics |
Crocetin meglumine has a molecular formula C21H29NO9 (MW 439.46 for the meglumine salt; crocetin free acid MW 328.40). The meglumine salt form increases aqueous solubility and oral bioavailability. The compound shows moderate plasma half-life and good brain penetration (BBB crossing). It is stored as a solid at 4degC, protected from light.
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| Toxicity/Toxicokinetics |
Crocetin meglumine is generally considered non-toxic at research doses. Preclinical studies show a wide safety margin. As a natural product derivative, it is well-tolerated. Standard safety studies are recommended for high-dose or long-term administration. It is for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
Crocetin meglumine is a research-grade compound derived from saffron (Crocus sativus L.). It is supplied as a solid with purity typically ≥98% (by HPLC). The compound is stored at 4degC, sealed and protected from light. It is soluble in DMSO (10 mM stock solution) and can be diluted in PBS for in vivo studies.
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| Molecular Formula |
C34H58N2O14
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| Molecular Weight |
718.83
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| Related CAS # |
Crocetin disodium;591230-99-8;Crocetin;27876-94-4
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| Appearance |
Typically exists as solid at room temperature
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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, avoid exposure to moisture. |
| 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 :~8.33 mg/mL (~11.59 mM )
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (1.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3911 mL | 6.9557 mL | 13.9115 mL | |
| 5 mM | 0.2782 mL | 1.3911 mL | 2.7823 mL | |
| 10 mM | 0.1391 mL | 0.6956 mL | 1.3911 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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