| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Geraniin targets TNF-α (tumor necrosis factor alpha), functioning as a TNF-α release inhibitor with an IC50 of 43 μM. It also targets oxidative stress pathways as an antioxidant. The compound has anti-tumor, anti-inflammatory, anti-oxidant, and anti-hyperglycemic activities. It is an ACE inhibitor useful for hypertension treatment. Geraniin has diverse biological activities including anticancer, anti-inflammatory, and liver protection.
|
|---|---|
| ln Vitro |
Geraniin has an IC50 value of 43 μM for blocking TNF-α release[1]. Throughout this time, geraniin has been utilized as a botanical remedy for a range of conditions, such as antihyperglycemic, anticancer, and anti-inflammatory effects. OVCAR3 and SKOV3 cell viability was dramatically decreased by geraniin in a concentration-dependent way. Geranol treatment resulted in IC50 values of 34.5±2.8 μM in OVCAR3 cells and 23.6±1.9 μM in SKOV3 cells. However, utilizing up to the maximum dose (80 μM) of geranol, treatment with 10 and 40 μM for 48 hours led to a substantial increase in cell fluorescence compared with normal versus control OVCAR3 cells (3.9 ± 1.1%). 22.6±1.4%) and 16.8±1.2%. Comparable outcomes were noted in SKOV3 cells [2].
In vitro, Geraniin has significant antioxidant activity. It is a TNF-α release inhibitor with an IC50 of 43 μM. The compound scavenges DPPH free radicals. It inhibits the growth of cancer cells, modulates oxidative stress, and suppresses inflammatory pathways. Geraniin protects PC12 cells against neuronal damage and may be used in the treatment of Alzheimer's disease. It is also an ACE inhibitor useful for hypertension treatment. |
| ln Vivo |
In comparison to acid treatment, geranol treatment postponed the formation of tumors, decreasing the percentage of tumor-bearing mice from 80.0% to 40.0% and the average number of tumors per mouse at week 20 from 3.8 to 1.1. Additionally, a schematic diagram demonstrated how geranin (50 mg/kg/d or 100 mg/kg/d) inhibited the activities of glutamic acid pyruvate aminotransferase, glutamic acid oxalopyruvate aminotransferase, starch esters, and total starch when treated with peroxidized oil[1].
In vivo, Geraniin has a protective effect against OVX-induced rat osteoporosis. It protects against neuronal damage. The compound has potential therapeutic applications in liver protection, cardiovascular health, and neuroprotection. Its anti-tumor, anti-inflammatory, antioxidant, and anti-hyperglycemic activities have been demonstrated in preclinical studies. Further in vivo studies are ongoing to fully characterize its therapeutic potential. |
| Enzyme Assay |
In vitro enzyme assays for Geraniin involve measuring TNF-α release inhibition. TNF-α levels are measured by ELISA in cell culture supernatants. The compound's IC50 of 43 μM is determined through dose-response curves. Antioxidant activity is assessed using DPPH free radical scavenging assays. ACE inhibition is measured using standard ACE activity assays. Anti-tumor activity is evaluated by assessing cancer cell proliferation inhibition. Assays are performed in appropriate buffer systems with positive controls such as known TNF-α inhibitors.
|
| Cell Assay |
In vitro cell-based assays for Geraniin are conducted in various cell lines including PC12 neuronal cells and cancer cells. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. TNF-α release is measured by ELISA. Cell viability is assessed by MTT or CCK-8 assays. Neuroprotection is assessed in PC12 cells exposed to neuronal damage. Antioxidant activity is assessed by measuring intracellular ROS levels. Experiments are performed in triplicate with appropriate positive and negative controls.
|
| Animal Protocol |
Geraniin in vivo studies are conducted in animal models of osteoporosis, neurodegeneration, and cancer. Animals are treated with Geraniin via oral administration or injection. For osteoporosis studies, OVX-induced rat models are used and bone density is measured. For neuroprotection studies, animal models of Alzheimer's disease are used. For cardiovascular studies, hypertension models are used. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
|
| ADME/Pharmacokinetics |
Geraniin (MW 952.6-952.64 g/mol, C41H28O27) is a hydrolysable polyphenol. It is soluble in DMSO at 100 mg/mL (104.97 mM). For in vivo administration, it can be formulated as a homogeneous suspension in CMC-Na at ≥5 mg/mL. The compound has a purity of 99.95%. Geraniin is a TNF-α release inhibitor with antioxidant, anticancer, and anti-inflammatory activities.
|
| Toxicity/Toxicokinetics |
Geraniin is generally well-tolerated in preclinical studies. The compound is a natural polyphenol with established safety profiles. Its anti-tumor, anti-inflammatory, antioxidant, and anti-hyperglycemic activities have been demonstrated with acceptable safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
|
| References |
|
| Additional Infomation |
Geraniin is a tannic acid. Geraniin has been found in Euphorbia pekinensis, Phyllanthus urinaria, and other organisms with available data.
Geraniin is a hydrolysable polyphenol and ellagitannin from Nephelium lappaceum fruit rind and Geranium species. It is a TNF-α release inhibitor (IC50 = 43 μM) with significant antioxidant activity. The compound has anti-tumor, anti-inflammatory, anti-oxidant, and anti-hyperglycemic activities. It protects against osteoporosis and neuronal damage and is an ACE inhibitor. All applications are limited to non-human research use. |
| Molecular Formula |
C41H28O27
|
|---|---|
| Molecular Weight |
952.6448
|
| Exact Mass |
952.081
|
| CAS # |
60976-49-0
|
| PubChem CID |
3001497
|
| Appearance |
Off-white to yellow solid powder
|
| Density |
2.3±0.1 g/cm3
|
| Index of Refraction |
1.948
|
| LogP |
3.41
|
| Hydrogen Bond Donor Count |
14
|
| Hydrogen Bond Acceptor Count |
27
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
68
|
| Complexity |
2080
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C1[C@@H]2[C@@H]3[C@@H]([C@H]([C@@H](O2)OC(=O)C4=CC(=C(C(=C4)O)O)O)OC(=O)C5=CC(=C(C6=C5[C@@H]7C(=CC(=O)[C@@](C7(O)O)(O6)O)C(=O)O3)O)O)OC(=O)C8=CC(=C(C(=C8C9=C(C(=C(C=C9C(=O)O1)O)O)O)O)O)O
|
| InChi Key |
JQQBXPCJFAKSPG-SVYIMCMUSA-N
|
| InChi Code |
InChI=1S/C41H28O27/c42-13-1-8(2-14(43)24(13)48)34(54)67-39-33-32-30(64-38(58)12-6-19(47)41(61)40(59,60)23(12)22-11(37(57)66-33)5-17(46)27(51)31(22)68-41)18(63-39)7-62-35(55)9-3-15(44)25(49)28(52)20(9)21-10(36(56)65-32)4-16(45)26(50)29(21)53/h1-6,18,23,30,32-33,39,42-46,48-53,59-61H,7H2/t18-,23+,30-,32+,33-,39+,41+/m1/s1
|
| Chemical Name |
[(1R,7R,8S,26R,28S,29R,38R)-1,13,14,15,18,19,20,34,35,39,39-undecahydroxy-2,5,10,23,31-pentaoxo-6,9,24,27,30,40-hexaoxaoctacyclo[34.3.1.04,38.07,26.08,29.011,16.017,22.032,37]tetraconta-3,11,13,15,17,19,21,32,34,36-decaen-28-yl] 3,4,5-trihydroxybenzoate
|
| 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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~104.97 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.62 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 25.0 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: ≥ 2.5 mg/mL (2.62 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 25.0 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: ≥ 2.5 mg/mL (2.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0497 mL | 5.2486 mL | 10.4971 mL | |
| 5 mM | 0.2099 mL | 1.0497 mL | 2.0994 mL | |
| 10 mM | 0.1050 mL | 0.5249 mL | 1.0497 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
