| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The primary target of 4alpha-PDD is the transient receptor potential vanilloid 4 (TRPV4) channel, a non-selective cation channel that is activated by a variety of physical and chemical stimuli. TRPV4 is involved in numerous physiological processes, including osmoregulation, mechanosensation, and thermoregulation. 4alpha-PDD acts as a direct agonist of TRPV4, binding to the channel and inducing its opening, which leads to an influx of calcium ions (Ca²⁺) into the cell. It is important to note that 4alpha-PDD is inactive for signaling through PKC, distinguishing it from other phorbol esters such as PMA.
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| ln Vitro |
4alpha-PDD is used in vitro as a pharmacological tool to activate TRPV4 channels. Its activation of TRPV4 leads to an increase in intracellular calcium concentration, which can be measured using calcium-sensitive fluorescent dyes such as Fura-2 or Fluo-4. The compound has been used to study the effects of TRPV4 activation in various cell types, including Madin-Darby canine kidney (MDCK) cells. Its specificity for TRPV4 over PKC makes it particularly useful for dissecting TRPV4-mediated signaling pathways without the interference of PKC-dependent effects. However, quantitative IC50 or EC50 data for TRPV4 activation are not extensively reported in the available literature.
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| ln Vivo |
In vivo data for 4alpha-PDD are limited, as the compound is primarily used as an in vitro research tool. However, TRPV4 agonists have been studied in various animal models to investigate the role of TRPV4 in pain, inflammation, and cardiovascular function. As a TRPV4 agonist, 4alpha-PDD could potentially be used in vivo to study TRPV4-mediated physiological responses. Its lack of PKC activity makes it a more specific tool for in vivo studies compared to other phorbol esters. However, specific in vivo efficacy data and experimental protocols for 4alpha-PDD are not detailed in the available literature.
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| Enzyme Assay |
In vitro assays for 4alpha-PDD typically involve measuring intracellular calcium concentrations in cells expressing TRPV4. Cells are loaded with a calcium-sensitive fluorescent dye, such as Fura-2 AM or Fluo-4 AM, and then stimulated with varying concentrations of 4alpha-PDD. The change in fluorescence intensity, which correlates with intracellular calcium levels, is monitored using a fluorescence microscope or a plate reader. The compound's activity is assessed by its ability to induce a concentration-dependent increase in intracellular calcium. This assay is used to confirm TRPV4 activation and to study the pharmacology of TRPV4 channels.
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| Cell Assay |
Cellular assays for 4alpha-PDD are performed in various cell lines that endogenously or exogenously express TRPV4. Cells are plated in multi-well plates and loaded with a calcium-sensitive fluorescent dye. After loading, the cells are treated with 4alpha-PDD at various concentrations, and the fluorescence signal is recorded in real-time. The increase in intracellular calcium is used as a readout of TRPV4 activation. Control experiments with known TRPV4 antagonists, such as RN-1734 or HC-067047, can be performed to confirm the specificity of the response. This assay is widely used to study TRPV4 channel function and pharmacology.
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| Animal Protocol |
In vivo animal studies with 4alpha-PDD are not extensively documented in the available literature. As a TRPV4 agonist, it could be used in rodent models to study TRPV4-mediated physiological and pathophysiological processes. For example, TRPV4 agonists have been used to study pain, inflammation, and vascular function. However, specific protocols for 4alpha-PDD administration, including routes of administration, dosing regimens, and experimental endpoints, are not detailed in the available sources. Researchers would need to consult the primary literature for specific in vivo protocols.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 4alpha-PDD are not extensively reported. The compound has a molecular weight of 672.93 and a density of 1.14 g/cm³. It is a phorbol ester, a class of compounds known for their lipophilic properties. The compound is typically dissolved in DMSO for in vitro studies. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Toxicological data for 4alpha-PDD are limited. As a phorbol ester, it belongs to a class of compounds that can have tumor-promoting activities. However, 4alpha-PDD is distinguished by its inactivity at PKC, which is the primary target for the tumor-promoting effects of many phorbol esters. The compound is classified as a research-use-only chemical and is not intended for human consumption. Specific toxicological data, including acute toxicity, genotoxicity, and carcinogenicity, are not reported in the available literature.
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| References |
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| Additional Infomation |
4α-Phorbolol 12,13-didecanoate is a phorbolol ester whose structure involves the conversion of the hydroxyl groups at the phorbolol cyclopropane linker (position 13) and the adjacent carbon atom (position 12) into the corresponding decanoate ester. It is a TRPV4-specific ligand and acts as a TRPV4 agonist. It is a phorbolol ester, decanoate ester, tertiary α-hydroxy ketone, diester, and primary allyl alcohol.
4alpha-PDD is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying TRPV4 channel function. Its specificity for TRPV4 over PKC makes it a unique and valuable reagent for dissecting TRPV4-mediated signaling pathways. The compound is used to study the role of TRPV4 in various physiological and pathophysiological processes, including pain, inflammation, and cardiovascular function. It is also used as a negative control for PKC-activating phorbol esters like PDD and PMA. |
| Molecular Formula |
C40H64O8
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|---|---|
| Molecular Weight |
672.94
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| Exact Mass |
672.46
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| CAS # |
27536-56-7
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| Related CAS # |
27536-56-7;
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| PubChem CID |
452544
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| Appearance |
White to off-white solid powder
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| Density |
1.14g/cm3
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| Boiling Point |
734.2ºC at 760mmHg
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| Flash Point |
212.4ºC
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| Vapour Pressure |
6.92E-25mmHg at 25°C
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| Index of Refraction |
1.546
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| LogP |
7.313
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
48
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| Complexity |
1220
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CCCCCCCCCC(=O)O[C@@H]1[C@H]([C@]2([C@@H](C=C(C[C@@]3([C@H]2C=C(C3=O)C)O)CO)[C@H]4[C@@]1(C4(C)C)OC(=O)CCCCCCCCC)O)C
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| InChi Key |
DGOSGFYDFDYMCW-OEFRVDPMSA-N
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| InChi Code |
InChI=1S/C40H64O8/c1-7-9-11-13-15-17-19-21-32(42)47-36-28(4)39(46)30(24-29(26-41)25-38(45)31(39)23-27(3)35(38)44)34-37(5,6)40(34,36)48-33(43)22-20-18-16-14-12-10-8-2/h23-24,28,30-31,34,36,41,45-46H,7-22,25-26H2,1-6H3/t28-,30+,31-,34-,36-,38+,39-,40-/m1/s1
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| Chemical Name |
4alpha-Phorbol 12,13-Didecanoate
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| Synonyms |
4α-Phorbol 12,13-didecanoate4alphaPDD4alpha-PDD 4alpha PDD
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4860 mL | 7.4301 mL | 14.8602 mL | |
| 5 mM | 0.2972 mL | 1.4860 mL | 2.9720 mL | |
| 10 mM | 0.1486 mL | 0.7430 mL | 1.4860 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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