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Isorhynchophylline is an alkaloid isolated from Crocus sativus with anticancer, antihypertensive, anti-inflammatory, and neuroprotective properties. Isorhynchophylline can be applied to cardiovascular and neurological disorders, and cancer studies.
Isorhynchophylline is an alkaloid isolated from Crocus sativus with anticancer, antihypertensive, anti-inflammatory, and neuroprotective properties. Isorhynchophylline can be applied to cardiovascular and neurological disorders, and cancer studies[1][2][3][4][5][6][7][8][9][10][11][12][13].
Cellular Effect
Cell Line
Type
Value
Description
References
HL-60
IC50
> 40 3
Compound: 6
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Isorhynchophylline (0.0625-40 µM, 48 h) shows cytotoxicity against human HL60 cells and SW480 cells (MTT assay), with IC50s greater than 40 μM[1].
Isorhynchophylline (3-15 µg/mL, 48 h) inhibits LPS-stimulated NO release in rat cortical microglial cells assessed as nitrite accumulation[2].
Isorhynchophylline (0.1-10.0 μM, 24 h) effectively inhibits angiotensin II-induced proliferation in rat vascular smooth muscle cells, at least in part, due to increased NO production and regulation of the cell cycle[3].
Isorhynchophylline (0-300 μM, 48 h) exerts anticancer and anti-metastatic effects through regulation of multiple signaling cascades (abatement of phospho-p38, etc.) in hepatocellular carcinoma cells [4].
Isorhynchophylline (1-50 μM, 2 h) protects PC12 cells against Beta-Amyloid-induced apoptosis via PI3K/Akt signaling pathway[5].
Isorhynchophylline (1-80 μM, 24 h) attenuates proliferation and migration of synovial fibroblasts via the FOXC1/β-catenin axis[6].
Isorhynchophylline (5-200 μM, 48 h) alleviates cartilage degeneration in osteoarthritis by activating autophagy in chondrocytes[7].
Isorhynchophylline (30 μM, 24 h) relieves ferroptosis-induced nerve damage after intracerebral hemorrhage via miR-122-5p/TP53/SLC7A11 pathway in hippocampal HT-22 cells[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rat vascular smooth muscle cells treated with Ang II (1.0 μM)
Concentration:
0.1, 1, 10 μM
Incubation Time:
24 h
Result:
Attenuated Ang II-induced cell proliferation in a concentration-dependent manner.
Abolished Ang-II induced VMSC proliferation at the highest concentration (10 μM).
Rat vascular smooth muscle cells treated with Ang II (1.0 μM)
Concentration:
0.1, 1, 10 μM
Incubation Time:
24 h
Result:
Suppressed the overexpression of c-fos mRNA in a concentration-dependent manner.
Decreased the over-expression of OPN and PCNA mRNA at 1.0 μM and 10.0 μM.
体内実験
Isorhynchophylline (20-40 mg/kg, i.g., daily, 8 weeks) ameliorates D-galactose (HY-N0210)-induced learning and memory deficits in mice, at least in part, by enhancing the antioxidant status and anti-inflammatory effects of brain tissue through inhibition of NFκB signaling[9].
Isorhynchophylline (50 μM, the first day of every week from the 5th to the 8th week after surgery) alleviates osteoarthritis in rat osteoarthritis models, with decreasing OARSI score and the reduction of joint space[7].
Isorhynchophylline (10-40 mg/kg, i.g., 7 days) exerts antidepressant-like effects in mice at least in part by inhibiting monoamine oxidase[10].
Isorhynchophylline (20-40 mg/kg, i.g., daily, 8 weeks) alleviates learning and memory impairments induced by aluminum chloride in mice[11].
Isorhynchophylline (20 mg/kg, i.p., 14 or 42 days) alleviates silicon-dioxide-induced lung injury in mice, with reducing inflammatory responses and fibrosis[12].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
D-galactose-induced cognitive deficits (Ten-week-old male ICR mice received a daily subcutaneous injection of D-gal at a dose of 100 mg/kg for 8 weeks)[9]
Dosage:
20, 40 mg/kg
Administration:
Given intragastrically (i.g.), daily, 8 weeks
Result:
Shortened the mean latency to find the platform at the 4th day (20 mg/kg).
Led to a significant increase in the number of target crossings (40 mg/kg).
Attenuated oxidative stress (enhanced the level of GSH, attenuated MDA).
Decreased the production of NO and the mRNA expression of iNOS in the brain (40 mg/kg).
Decreased the production of PGE2 and the mRNA expression of COX-2 (40 mg/kg).
Suppressed the protein level of p-IκBα (40 mg/kg).
Room temperature in continental US; may vary elsewhere.
保管条件
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (260.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.6010 mL
13.0049 mL
26.0098 mL
5 mM
0.5202 mL
2.6010 mL
5.2020 mL
10 mM
0.2601 mL
1.3005 mL
2.6010 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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