| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
| Targets |
Geniposide targets multiple pathways and molecules involved in inflammation, apoptosis, and oxidative stress. Its anti-apoptotic activity is due to modulation of p53, Bax, Bcl-2, and Caspase-3-related factors. The compound's neuroprotective effects are mediated through its ability to reduce oxidative stress and inflammation. Its antithrombotic, anti-inflammatory, and antidiabetic activities involve modulation of various signaling pathways. The compound's specific molecular targets are being elucidated through ongoing research.
|
|---|---|
| ln Vitro |
Anti-thrombotic, anti-inflammatory, anti-diabetic, anti-atherosclerotic, anti-depressant, anti-hypertensive, toxicological, and adverse reaction properties are just a few of the actions of geniposide [1]. The production of IL-8, IL-1β, and MCP-1 in brain microvascular endothelial cells induced by OGD is significantly reduced by geniposide. This results in a significant inhibition of P2Y14 receptor expression and phosphorylation of RAF-1, MEK1/2, and ERK1/2[2].
Geniposide exhibits a variety of in vitro activities including antithrombotic, anti-inflammatory, anti-diabetic, anti-atherosclerotic, antidepressant, and neuroprotective effects. It significantly reduces IL-8 production. The compound's anti-apoptotic activity is mediated through modulation of p53, Bax, Bcl-2, and Caspase-3. Its antioxidant and antiproliferative activities have been demonstrated in various cell lines. The compound's effects on Alzheimer's disease-related pathology have been observed in vitro. |
| ln Vivo |
In a dose-dependent way, geniposide (200 and 400 mg/kg) dramatically lowered insulin, TG, and blood glucose levels in diabetic patients. A considerable reduction in alcohol-induced blood ALT/AST and excessive rise of liver LPO levels can be achieved by using geniposide (20.0, 40.0, or 80 mg/kg), which also lowers immune protein response levels and GP and G6Pase expression at mRNA levels. By increasing the production of heme oxygenase-1 (HO-1), geniposide alleviates the transplantation-induced stress on primary cultured hippocampus neuron cells caused by 3-modenoimine hydrochloride (SIN-1) [4]. prevents IκB from degrading and turns into an extremely powerful NF-κB coupling [1].
Geniposide (100 mg/kg) prevents increases in apoptosis and decreases in the number of dopaminergic neurons in the substantia nigra in a mouse model of MPTP-induced Parkinson's disease. The compound is highly effective in inhibiting acute lung injury and may be a promising therapeutic reagent for acute lung injury treatment. Its neuroprotective, hepatoprotective, antithrombotic, and anti-inflammatory effects have been demonstrated in various in vivo models. |
| Enzyme Assay |
In vitro enzyme assays for geniposide involve measuring its effects on enzymes involved in inflammation and oxidative stress. The compound's antioxidant activity is assessed using standard cell-free assays such as DPPH radical scavenging, ABTS, or FRAP. Its anti-inflammatory activity can be evaluated by measuring inhibition of inflammatory enzymes such as COX-2 or iNOS. The compound's effects on apoptosis-related proteins can be assessed using purified proteins or cell lysates. These assays provide mechanistic insights into the compound's biological activities.
|
| Cell Assay |
In vitro cell-based assays for geniposide involve treating various cell lines (neuronal cells, immune cells, cancer cells) with the compound to assess its effects on cell viability, apoptosis, inflammation, and oxidative stress. Apoptosis is quantified by measuring caspase activity, Bax/Bcl-2 ratio, and p53 expression. Cytokine production (IL-8, TNF-α, IL-6) is measured by ELISA. Oxidative stress is assessed by measuring reactive oxygen species levels and antioxidant enzyme activities. Cell viability is measured using MTT or similar assays. These cellular studies characterize the compound's pharmacological activities.
|
| Animal Protocol |
In vivo animal experiments for geniposide have been conducted in mouse models of MPTP-induced Parkinson's disease. Mice are treated with geniposide (100 mg/kg) and dopaminergic neuron loss and apoptosis in the substantia nigra are assessed. Acute lung injury models evaluate the compound's anti-inflammatory effects. Models of diabetes, depression, and Alzheimer's disease have also been used to assess efficacy. Efficacy endpoints include histopathological analysis, biomarker measurement, and behavioral assessments.
|
| ADME/Pharmacokinetics |
Geniposide has a molecular weight of 388.37 and a molecular formula of C17H24O10. It is an iridoid glycoside with good aqueous solubility due to its glycosidic structure. The compound is typically extracted from fruit sources. Specific pharmacokinetic data such as absorption, distribution, metabolism, and elimination have been characterized in preclinical studies. The compound is typically stored under recommended conditions for natural products.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for geniposide is not extensively reported. As a natural compound from fruit sources with a history of use in traditional medicine, it is generally considered to have a favorable safety profile. However, toxicological effects and adverse reactions have been summarized in the literature. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound in research settings.
|
| References |
|
| Additional Infomation |
Geniposide is a terpene glycoside. It has been reported to be found in Rehmannia glutinosa, Gardenia jasminoides, and other organisms with relevant data. See also: Gardenia jasminoides (whole plant, part).
Geniposide is an iridoid glycoside with diverse biological activities including neuroprotective, anti-diabetic, antiproliferative, antioxidative, anti-inflammatory, and anti-apoptotic effects. It modulates p53, Bax, Bcl-2, and Caspase-3 in its anti-apoptotic activity. Geniposide has therapeutic potential for Parkinson's disease, acute lung injury, Alzheimer's disease, and metabolic disorders. The compound is a major iridoid found in fruit and is used in Asian traditional medicine. |
| Molecular Formula |
C17H24O10
|
|---|---|
| Molecular Weight |
388.37
|
| Exact Mass |
388.136
|
| CAS # |
24512-63-8
|
| PubChem CID |
107848
|
| Appearance |
White to yellow solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
641.4±55.0 °C at 760 mmHg
|
| Melting Point |
161-162ºC
|
| Flash Point |
231.5±25.0 °C
|
| Vapour Pressure |
0.0±4.3 mmHg at 25°C
|
| Index of Refraction |
1.621
|
| LogP |
-1.92
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
617
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
COC(=O)C1=CO[C@H]([C@H]2[C@@H]1CC=C2CO)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O
|
| InChi Key |
IBFYXTRXDNAPMM-BVTMAQQCSA-N
|
| InChi Code |
InChI=1S/C17H24O10/c1-24-15(23)9-6-25-16(11-7(4-18)2-3-8(9)11)27-17-14(22)13(21)12(20)10(5-19)26-17/h2,6,8,10-14,16-22H,3-5H2,1H3/t8-,10-,11-,12-,13+,14-,16+,17+/m1/s1
|
| Chemical Name |
methyl (1S,4aS,7aS)-7-(hydroxymethyl)-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-carboxylate
|
| 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 : ~100 mg/mL (~257.49 mM)
H2O : ~50 mg/mL (~128.74 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.08 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 27.5 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: ≥ 2.75 mg/mL (7.08 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 27.5 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: ≥ 2.75 mg/mL (7.08 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: 100 mg/mL (257.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5749 mL | 12.8743 mL | 25.7486 mL | |
| 5 mM | 0.5150 mL | 2.5749 mL | 5.1497 mL | |
| 10 mM | 0.2575 mL | 1.2874 mL | 2.5749 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.