| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Dipeptidyl Peptidase-IV Inhibitor[2]
Dipeptidyl peptidase-IV (DPP-4) |
|---|---|
| ln Vitro |
Azaleatin functions as a DPP-4 inhibitor. This activity is central to its potential use in metabolic research. By inhibiting DPP-4, it may help to increase the half-life of incretin hormones like GLP-1, which play a key role in regulating insulin secretion and blood glucose levels.
|
| ln Vivo |
Currently, no specific in vivo data is available for this compound. General in vivo information for similar flavonoid DPP-4 inhibitors may include their ability to lower blood glucose levels in oral glucose tolerance tests and improve insulin sensitivity in rodent models of type 2 diabetes.
|
| Enzyme Assay |
A standard DPP-4 inhibition assay uses a fluorogenic substrate like Gly-Pro-AMC. The compound is pre-incubated with the DPP-4 enzyme in a buffer (e.g., 50 mM Tris-HCl, pH 7.4) at 37degC for 10 minutes. The reaction is initiated by adding the substrate, and fluorescence is measured (Ex/Em=380/460 nm) to calculate inhibition.
|
| Cell Assay |
General cellular protocols for flavonoid research may use Caco-2 or HepG2 cells. Cells are treated with the compound, and DPP-4 activity is measured in cell lysates. To assess functional effects, insulin secretion can be measured in pancreatic beta-cell lines (e.g., INS-1) treated with the compound in the presence of glucose and GLP-1.
|
| Animal Protocol |
General in vivo procedures for DPP-4 inhibitor research involve an oral glucose tolerance test in diabetic mice (e.g., db/db mice). Azaleatin is administered orally (e.g., 10-100 mg/kg) 30 minutes before an oral glucose challenge. Blood glucose is measured via tail-vein sampling at 0, 30, 60, and 120 minutes after glucose administration.
|
| ADME/Pharmacokinetics |
Azaleatin has a molecular weight of 316.26. As a flavonoid, it is expected to have low oral bioavailability due to poor water solubility and extensive first-pass metabolism (glucuronidation, sulfation). Its absorption and metabolism are typical for this class of polyphenolic natural products.
|
| Toxicity/Toxicokinetics |
Toxicity data for azaleatin is limited, but flavonoids are generally considered safe with low toxicity. In cell-based assays, it shows a good safety profile. No LD50 or specific organ toxicity has been reported. High doses may cause gastrointestinal distress due to general polyphenol properties.
|
| References | |
| Additional Infomation |
Azelin is a monomethoxyflavonoid, a compound formed by replacing the 5-hydroxyl group of quercetin with a methoxy group. It is a plant metabolite. It is a 7-hydroxyflavone, a tetrahydroxyflavonoid, and a monomethoxyflavonoid. Its function is related to that of quercetin. Azelin has been reported to be found in Rhododendron species (such as Rhododendron dauricum and Rhododendron latushii) and other organisms with relevant data.
Azaleatin is a natural product-based research tool. Its classification as a DPP-4 inhibitor suggests potential applications in studying type 2 diabetes and obesity. It is not an approved drug and has not progressed to clinical trials. It is used as a lead compound for drug discovery or as a reference standard for phytochemical analysis. |
| Molecular Formula |
C16H12O7
|
|---|---|
| Molecular Weight |
316.26
|
| Exact Mass |
316.058
|
| CAS # |
529-51-1
|
| PubChem CID |
5281604
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.634g/cm3
|
| Boiling Point |
657.3ºC at 760mmHg
|
| Flash Point |
250.2ºC
|
| Index of Refraction |
1.74
|
| Source |
Originated from plants: Compositae Carthamus tinctorius L.
|
| LogP |
2.291
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
23
|
| Complexity |
503
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC(=CC2=C1C(=O)C(=C(O2)C3=CC(=C(C=C3)O)O)O)O
|
| InChi Key |
RJBAXROZAXAEEM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H12O7/c1-22-11-5-8(17)6-12-13(11)14(20)15(21)16(23-12)7-2-3-9(18)10(19)4-7/h2-6,17-19,21H,1H3
|
| Chemical Name |
2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-5-methoxychromen-4-one
|
| 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) |
DMSO: ~50 mg/mL (~158.1 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% 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 DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 1.25 mg/mL (3.95 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 DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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 | 3.1620 mL | 15.8098 mL | 31.6196 mL | |
| 5 mM | 0.6324 mL | 3.1620 mL | 6.3239 mL | |
| 10 mM | 0.3162 mL | 1.5810 mL | 3.1620 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
