| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Podocarpic acid targets TRPA1 (Transient Receptor Potential Ankyrin 1) as a novel activator. It also targets LXRalpha and LXRbeta receptors through its anhydride form, acting as a 1 nM agonist. The compound increases ionic currents. Its mechanism involves modulation of TRPA1-mediated pain pathways and LXR-mediated lipid metabolism. Podocarpic acid has diverse biological activities.
|
|---|---|
| ln Vitro |
Podocarpic anhydride agonistically interacts with LXRα and β receptors at 1 nM.It is more than 8–10 times more efficient than one of the natural ligands, 22–(R)–hydroxycholesterol, as an LXR receptor activator in HEK-293 cells [2].
In vitro, Podocarpic acid is a natural product that acts as a novel TRPA1 activator. At 20 µM, it reduces hyperesthesia and neuronal damage. Podocarpic acid anhydride acts as a 1 nM agonist of LXRalpha and beta receptors. The compound increases ionic currents. Its diverse biological activities have been characterized in various cell-based and tissue-based assays. |
| ln Vivo |
SKN-1 in C is activated by mogrosanic acid. elegans, making it comparable to well-known Nrf2 activators like LA. Additionally, SKN-1 activation produced by mohenate or LA requires TRPodocarpic Acid-1; in glod-4;gst-4p::gfp mice, trPodocarpic Acid-1 knockdown restored gst-4 expression to wild-type levels. The strong Ca2+ flux that was induced by supplementing with A and LA was greatly diminished when the Ca2+-impermeable TRPodocarpic Acid-1E1018A channel was present, suggesting that TRPodocarpic Acid-1 activation is essential for the therapeutic effects of these agents. Ultimately, high endogenous MGO and GO were restored to levels almost identical to wild type by podocarpus acid and LA, which mitigated the podocarbin acidogenic phenotype of glod-4 animals [1].
In vivo, Podocarpic acid reduces hyperesthesia, neuronal damage, and increases lifespan in a model of α-dicarbonyl-related stress using C. elegans. As a TRPA1 activator, it has potential for pain management research. The compound is a natural product with promising therapeutic applications. Further in vivo studies are ongoing to fully characterize its therapeutic potential. The compound is typically administered orally or via injection in preclinical studies. |
| Enzyme Assay |
In vitro receptor binding assays for Podocarpic acid involve measuring TRPA1 activation. TRPA1 activity is assessed by measuring calcium influx in cells expressing TRPA1 using fluorescence-based assays. LXRalpha and LXRbeta activation is assessed using reporter gene assays. For neuronal protection studies, neuronal cells are treated with the compound and cell viability and neuronal damage are assessed. Assays are performed in appropriate buffer systems with positive controls such as known TRPA1 activators.
|
| Cell Assay |
In vitro cell-based assays for Podocarpic acid are conducted in neuronal cells and cells expressing TRPA1 or LXR receptors. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. TRPA1 activation is assessed by measuring calcium influx. LXR activation is assessed by measuring target gene expression. Cell viability is assessed by standard assays. Neuroprotection is assessed in models of oxidative stress or excitotoxicity. Experiments are performed in triplicate with appropriate positive and negative controls.
|
| Animal Protocol |
Podocarpic acid in vivo studies are conducted in animal models of pain and neurodegenerative diseases. Animals are treated with Podocarpic acid via oral administration or injection. For pain studies, hyperesthesia is assessed using standard pain models. For neuroprotection studies, animal models of neurodegeneration are used. For lifespan studies, C. elegans models are used. Dosing regimens are optimized based on pharmacokinetic data. 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 |
Podocarpic acid (MW 274.35 g/mol, C17H22O3) is a naturally occurring diterpenoid. It is found in D. cupressinum resins. The compound is a solid with a purity of 99.67%. It is soluble in organic solvents. It is stable under recommended storage conditions. Podocarpic acid is a novel TRPA1 activator and LXR agonist. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
|
| Toxicity/Toxicokinetics |
Podocarpic acid is generally well-tolerated in preclinical studies. The compound is a natural diterpenoid with established safety profiles. Its TRPA1 activating and neuroprotective effects 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 |
Podocarpic acid is a diterpenoid compound without an isopropyl substituent, possessing an aromatic C-ring and a hydroxyl group at position 12. It is derived from the hydride of Podocarpic. Podocarpic acid has been reported to exist in Podocarpic totara, Dacrycarpus dacrydioides, and other organisms with relevant data.
Podocarpic acid is a naturally occurring diterpenoid from D. cupressinum resins that acts as a novel TRPA1 activator and reduces hyperesthesia and neuronal damage. Its anhydride form acts as a 1 nM agonist of LXRalpha and beta receptors. The compound increases ionic currents and increases lifespan in a stress model. Its molecular formula is C17H22O3 with a molecular weight of 274.35 g/mol. All applications are limited to non-human research use. |
| Molecular Formula |
C17H22O3
|
|---|---|
| Molecular Weight |
274.35478
|
| Exact Mass |
274.157
|
| CAS # |
5947-49-9
|
| PubChem CID |
93017
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
193-196 ℃(lit.)
|
| LogP |
3.487
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
407
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@]12CCC[C@]([C@@H]1CCC3=C2C=C(C=C3)O)(C)C(=O)O
|
| InChi Key |
VJILEYKNALCDDV-OIISXLGYSA-N
|
| InChi Code |
InChI=1S/C17H22O3/c1-16-8-3-9-17(2,15(19)20)14(16)7-5-11-4-6-12(18)10-13(11)16/h4,6,10,14,18H,3,5,7-9H2,1-2H3,(H,19,20)/t14-,16-,17+/m1/s1
|
| Chemical Name |
(1S,4aS,10aR)-6-hydroxy-1,4a-dimethyl-2,3,4,9,10,10a-hexahydrophenanthrene-1-carboxylic acid
|
| 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 (~364.50 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.58 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 (7.58 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 (7.58 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 | 3.6450 mL | 18.2249 mL | 36.4498 mL | |
| 5 mM | 0.7290 mL | 3.6450 mL | 7.2900 mL | |
| 10 mM | 0.3645 mL | 1.8225 mL | 3.6450 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
