| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: =99.73%
| Targets |
Proto - oncogene kinase Pim - 1 (IC50 = 2.71 μM)
Phosphatidylinositol 3 - kinase (PI3K)、Akt AMP - activated protein kinase (AMPK) |
|---|---|
| ln Vitro |
HispiduLin causes dose- and time-dependent cell death in HepG2 cells. Through mitochondrial function, hispiduLin causes cellular problems that are typified by increased release of pigment C and activated Capase-3, disturbance of the potential of the mitochondrial membrane, and reduced Bcl-2/Bax [2].
Hispidulin shows inhibitory activity against Pim - 1 kinase. In HepG2 cancer cells, hispidulin induces apoptosis in a dose - and time - dependent manner. It causes mitochondrial dysfunction, characterized by a decreased Bcl - 2/Bax ratio, disrupted mitochondrial membrane potential, and increased release of cytochrome c and activation of caspase - 3. It also inhibits the PI3K/Akt signaling pathway. |
| ln Vivo |
The size of mice tumors is significantly inhibited by HispiduLin [2]. Treatment with HispiduLin effectively reduces bone loss from late resection and stops weight loss from ovariectomy. Treatment with HispiduLin also decreased ovariectomy trabeculae. Thirty minutes before to intraperitoneal injection of HispiduLin (10 or 50 mg/kg), kainic acid (15 mg/kg) infusion increased the predicted incubation period and decreased prediction scores. Moreover, HispiduLin has far less data. Hippocampal neuronal cell death is caused by radotoxin, and this protective effect is accompanied by pro-inflammatory cytokines such apoptotic factor-α, interleukin-1β, and interleukin-6, as well as tumor suppression by astrocyte activators[4].
In ovariectomized mice, hispidulin exerts anti - osteoporotic activity by activating the AMPK signaling pathway, which can mitigate body and bone loss and reduce trabecular spacing. In a rat model of kainic acid - induced seizures, hispidulin (10 or 50 mg/kg) is administered intraperitoneally 30 minutes before kainic acid injection (15 mg/kg). It can increase seizure latency, lower seizure scores, reduce hippocampal neuronal cell death, diminish microglial activation, and decrease the production of pro - inflammatory cytokines (interleukin - 1β, interleukin - 6, and tumor necrosis factor - α) in the hippocampus. |
| Cell Assay |
HepG2 cancer cells are cultured and treated with different concentrations of hispidulin for different time periods. Then, the expression levels of Bcl - 2, Bax, cytochrome c, and caspase - 3 are detected by Western blot. The mitochondrial membrane potential is measured using a mitochondrial membrane potential detection kit. Meanwhile, the activation status of the PI3K/Akt signaling pathway is evaluated by detecting the phosphorylation levels of related proteins through Western blot.
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| Animal Protocol |
For ovariectomized mice, hispidulin is dissolved in an appropriate solvent and administered to the mice, and the specific administration frequency is not mentioned. The experimental period is long - term, and finally, the body weight, bone mass, and trabecular structure of the mice are detected.
For rats, hispidulin is dissolved in an appropriate solvent and intraperitoneally injected at a dose of 10 or 50 mg/kg, 30 minutes before kainic acid injection (15 mg/kg). Then, the seizure latency and scores are recorded, and after the experiment, the hippocampal tissues are collected to detect neuronal cell death, microglial activation, and the levels of pro - inflammatory cytokines. |
| References |
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| Additional Infomation |
Hispidulin is a natural flavone with a broad spectrum of biological activities.
Hispidulin is a monomethoxyflavone that is scutellarein methylated at position 6. It has a role as an apoptosis inducer, an anti-inflammatory agent, an antioxidant, an anticonvulsant, an antineoplastic agent and a plant metabolite. It is a trihydroxyflavone and a monomethoxyflavone. It is functionally related to a scutellarein. Hispidulin (4',5,7-trihydroxy-6-methoxyflavone) is a potent benzodiazepine (BZD) receptor ligand with positive allosteric properties. Hispidulin has been reported in Salvia plebeia, Bejaranoa balansae, and other organisms with data available. See also: Arnica montana Flower (part of). |
| Molecular Formula |
C16H12O6
|
|---|---|
| Molecular Weight |
300.27
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| Exact Mass |
300.063
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| Elemental Analysis |
C, 64.00; H, 4.03; O, 31.97
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| CAS # |
1447-88-7
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| PubChem CID |
5281628
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
601.5±55.0 °C at 760 mmHg
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| Flash Point |
230.1±25.0 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.697
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
454
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C2=C(C=C1O)OC(=CC2=O)C3=CC=C(C=C3)O)O
|
| InChi Key |
IHFBPDAQLQOCBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H12O6/c1-21-16-11(19)7-13-14(15(16)20)10(18)6-12(22-13)8-2-4-9(17)5-3-8/h2-7,17,19-20H,1H3
|
| Chemical Name |
5,7-dihydroxy-2-(4-hydroxyphenyl)-6-methoxychromen-4-one
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| Synonyms |
NSC122415; NSC-122415; Hispidulin; 1447-88-7; Dinatin; Scutellarein 6-methyl ether; 4',5,7-Trihydroxy-6-methoxyflavone; 4H-1-BENZOPYRAN-4-ONE, 5,7-DIHYDROXY-2-(4-HYDROXYPHENYL)-6-METHOXY-; Salvitin; 5,7-dihydroxy-2-(4-hydroxyphenyl)-6-methoxychromen-4-one; NSC 122415; Dinatin; Hispidulin
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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 |
| 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 : ~62.5 mg/mL (~208.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (6.93 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (33.30 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3303 mL | 16.6517 mL | 33.3034 mL | |
| 5 mM | 0.6661 mL | 3.3303 mL | 6.6607 mL | |
| 10 mM | 0.3330 mL | 1.6652 mL | 3.3303 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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