Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
Neuron-like cell viability is not compromised by crocin-4 (0.1-1000 μM; 24-72 h)[1]. In SH-SY5Y-APP cells, crocin-4 (1 mM; 72 h) increases PSEN1-CTF and PSEN2, while reducing total PSEN1, PSEN1 and PSEN2 complexes, BACE1, APP -C99, and sAPPα[1]. In PC12-htau cells, crocin-4 (1 mM; 72 h) significantly lowers tau levels and phosphorylation on the pThr231 and pSer199/Ser202 epitopes[1]. It also suppresses GSK3β and ERK1/2 kinases.
|
---|---|
ln Vivo |
The blood brain barrier (BBB) can be crossed by crocin-4 (50 mg/kg; ip), which can then accumulate in the mouse brain[3].
|
Cell Assay |
Western Blot Analysis[1]
Cell Types: Differentiated SH-SY5Y-APP cells Tested Concentrations: 1 mM Incubation Duration: 72 hrs (hours) Experimental Results: Dramatically diminished total PSEN1 by 19%, and the PSEN1 and PSEN2 complexes by 81 and 65%, while it increased PSEN1-CTF (26%) and PSEN2 (43%). The key molecules of the amyloidogenic pathway, BACE1 and APP-C99 were Dramatically diminished by 20 and 28%, respectively. The non-amyloidogenic pathway product sAPPα was also decreased, by 44%, while APP-C83 remained unaltered. Western Blot Analysis[1] Cell Types: Differentiated PC12-htau cells Tested Concentrations: 1 mM Incubation Duration: 72 hrs (hours) Experimental Results: Dramatically diminished total tau levels (by 32%) and tau phosphorylation (pThr231 and pSer199/Ser202-tau by 22 and 75%, respectively). Downregulates the active and inactive forms of GSK3β (total GSK3β by 34%, pSer9- GSK3β by 30%) and ERK1/2 (total ERK2 by 37%, pERK1 by 40%, pERK2 by 50%). |
References |
[1]. Chalatsa I, et, al. The Crocus sativus Compounds trans-Crocin 4 and trans-Crocetin Modulate the Amyloidogenic Pathway and Tau Misprocessing in Alzheimer Disease Neuronal Cell Culture Models. Front Neurosci. 2019 Mar 26;13:249.
[2]. Koulakiotis NS, et, al. Crocus-derived compounds alter the aggregation pathway of Alzheimer's Disease: associated beta amyloid protein. Sci Rep. 2020 Oct 23;10(1):18150. [3]. Karkoula E, et, al. Trans-crocin 4 is not hydrolyzed to crocetin following i.p. administration in mice, while it shows penetration through the blood brain barrier. Fitoterapia. 2018 Sep;129:62-72. |
Molecular Formula |
C27H36O9
|
---|---|
Molecular Weight |
504.57
|
CAS # |
55750-86-2
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C/C(/C=C/C=C(/C(O[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)=O)\C)=C\C=C\C=C(\C=C\C=C(\C(O[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)=O)/C)/C
|
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 (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
---|---|
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 | 1.9819 mL | 9.9094 mL | 19.8189 mL | |
5 mM | 0.3964 mL | 1.9819 mL | 3.9638 mL | |
10 mM | 0.1982 mL | 0.9909 mL | 1.9819 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.