| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| Other Sizes |
| Targets |
iNOS
Irisflorentin targets the nitric oxide synthase (NOS) pathway, specifically reducing iNOS expression and NO production. It promotes rpn-3 expression to enhance proteasome activity and down-regulates egl-1 expression to block apoptosis pathways. The compound also exhibits estrogenic activity. |
|---|---|
| ln Vitro |
LPS-stimulated RAW 264.7 macrophage viability is unaffected by isisin at doses up to 40 μM [1]. In RAW 264.7 macrophages, irisflorentin (10–40 μM) suppresses LPS-induced NO generation in a concentration-dependent manner without changing iNOS activity [1]. LPS (10 ng/mL)-stimulated RAW 264.7 macrophages exhibit a rise in iNOS mRNA expression that is concentration-dependently inhibited by irisflorentin (10–40 μM). The production of TNF-α, IL-1β, and IL-6 in LPS-stimulated RAW 264.7 macrophages is concentration-dependently inhibited by irisflorentin (10–40 μM) [1]. LPS (10 ng/mL)-induced elevation of iNOS protein levels is inhibited concentration-dependently by irisflorentin (10–40 μM). A concentration-dependent effect of irisflorentin (10–40 μM) suppresses LPS-induced phosphorylation of p38 and ERK1/2, while having minimal effect on JNK phosphorylation [1].
In vitro, irisflorentin (10-40 μM) suppresses LPS-induced NO generation in a concentration-dependent manner in RAW 264.7 macrophages without changing iNOS activity. It markedly reduces the transcriptional and translational levels of iNOS. The compound exhibits estrogenic activity in human MCF7 cells, stimulating cell proliferation at an activity level of 50.3 μM, equivalent to that caused by 10 pM estradiol. |
| ln Vivo |
In vivo studies on irisflorentin are limited. Based on its anti-inflammatory activity, the compound may have potential in inflammatory disorders. Its ability to block apoptosis pathways suggests potential in conditions involving dysregulated apoptosis. Further in vivo studies are needed to fully characterize its pharmacological effects and therapeutic potential.
|
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, irisflorentin can be evaluated for iNOS inhibition. Cell-free assays using recombinant iNOS or macrophage lysates can be performed. The compound is incubated with iNOS enzyme and its substrate (L-arginine) in the presence of cofactors. Nitric oxide production is measured using the Griess reaction. IC₅₀ values are calculated from dose-response curves.
|
| Cell Assay |
RT-PCR[1]
Cell Types: LPS-stimulated RAW 264.7 macrophages Tested Concentrations: 10, 20, 40 μM Incubation Duration: Experimental Results: Inhibition of LPS (10 ng/mL)-induced increase in iNOS mRNA expression. Inhibits the production of TNF-α, IL-1β and IL-6. Western Blot Analysis [1] Cell Types: LPS-stimulated RAW 264.7 macrophages Tested Concentrations: 10, 20, 40 μM Incubation Duration: Experimental Results: Inhibition of LPS (10 ng/mL)-induced increase in iNOS protein levels. Inhibits LPS-induced phosphorylation of p38 and ERK1/2, but slightly affects JNK phosphorylation. For in vitro cell-based assays, irisflorentin is typically tested on RAW 264.7 macrophages. Cells are treated with the compound at various concentrations (10-40 μM) and stimulated with LPS. NO production in the culture medium is measured using the Griess reaction. iNOS expression is assessed by Western blotting or qPCR. Apoptosis-related protein expression is assessed by Western blotting. Estrogenic activity is evaluated in MCF7 cell proliferation assays. |
| Animal Protocol |
In vivo animal experiments for irisflorentin have not been extensively reported. Based on its anti-inflammatory activity, potential experimental models include inflammation models in mice or rats. The compound could be administered orally or intraperitoneally, with inflammatory markers assessed as pharmacodynamic endpoints.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for irisflorentin are limited. As an isoflavone, it is expected to have moderate oral bioavailability. The compound may undergo metabolism in the liver. Standard pharmacokinetic studies would be required to determine its absorption, distribution, metabolism, and excretion profile.
|
| Toxicity/Toxicokinetics |
Toxicological data for irisflorentin are limited. As a natural product isolate, it is generally considered to have low toxicity at pharmacological doses. However, comprehensive toxicological studies have not been extensively reported. The compound is classified as a research-grade reagent and is not for human use.
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| References | |
| Additional Infomation |
Irisin is a 4'-methoxyisoflavonoid compound. It has been reported to exist in Iris plants (such as Iris tectorum and Iris potaninii) and other organisms with relevant data.
Irisflorentin is a research-use only compound and has not been approved for clinical applications. It is also known as次野鸢尾黄素 in Chinese. The compound is a major active component in Rhizoma Belamcandae. Its molecular weight and formula are well-characterized. It is available from various research chemical suppliers. |
| Molecular Formula |
C20H18O8
|
|---|---|
| Molecular Weight |
386.3521
|
| Exact Mass |
386.1
|
| CAS # |
41743-73-1
|
| PubChem CID |
170569
|
| Appearance |
White to off-white solid
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
569.1±50.0 °C at 760 mmHg
|
| Melting Point |
169 °C
|
| Flash Point |
250.5±30.2 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.593
|
| LogP |
3.19
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
28
|
| Complexity |
593
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C([H])=C(C2C([H])=C(C(=C(C=2[H])OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H])C(C2=C(C3=C(C([H])=C12)OC([H])([H])O3)OC([H])([H])[H])=O
|
| InChi Key |
RISXUTCDCPHJFQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H18O8/c1-22-13-5-10(6-14(23-2)18(13)24-3)11-8-26-12-7-15-19(28-9-27-15)20(25-4)16(12)17(11)21/h5-8H,9H2,1-4H3
|
| Chemical Name |
9-methoxy-7-(3,4,5-trimethoxyphenyl)-[1,3]dioxolo[4,5-g]chromen-8-one
|
| Synonyms |
Irisflorentin
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~129.42 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5883 mL | 12.9416 mL | 25.8833 mL | |
| 5 mM | 0.5177 mL | 2.5883 mL | 5.1767 mL | |
| 10 mM | 0.2588 mL | 1.2942 mL | 2.5883 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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