4α-Phorbol 12,13-didecanoate
Based on 1 Customer Validation
4α-Phorbol 12,13-didecanoate (4αPDD) is a transient receptor potential vanilloid 4 (TRPV4) agonist. 4α-Phorbol 12,13-didecanoate can promote Ca2+ influx, induce ATP release and function as an osmoreceptor. 4α-Phorbol 12,13-didecanoate can inhibit water intake and increase maximal micturition pressure in rats. 4α-Phorbol 12,13-didecanoate can be used for the researches of inflammation and infection, such as chikungunya virus (CHIKV).
For research use only. We do not sell to patients.
- Purity: 99%
- CAS No.: 27536-56-7
- Formula: C40H64O8
- Molecular Weight:672.93
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Storage:Pure form -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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TRPV4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>6 μM
Compound: 2a, 4alpha-PDD
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Activation of mouse TRPV4 W586A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration
Activation of mouse TRPV4 W586A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration
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[PMID: 19361196] |
| HEK293 | EC50 |
0.32 μM
Compound: 2a, 4alpha-PDD
|
Activation of mouse TRPV4 S557A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration
Activation of mouse TRPV4 S557A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration
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[PMID: 19361196] |
| HEK293 | EC50 |
0.37 μM
Compound: 2a, 4alpha-PDD
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Activation of mouse wild type TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium concentration
Activation of mouse wild type TRPV4 expressed in HEK293 cells assessed as increase in intracellular calcium concentration
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[PMID: 19361196] |
| HEK293 | EC50 |
6.3 μM
Compound: 2a, 4alpha-PDD
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Activation of mouse TRPV4 Y556A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration
Activation of mouse TRPV4 Y556A mutant expressed in HEK293 cells assessed as increase in intracellular calcium concentration
|
[PMID: 19361196] |
| MT4 | EC50 |
>16 μM
Compound: 12
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Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay
Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay
|
[PMID: 25970561] |
| MT4 | EC50 |
>16 μM
Compound: 12
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Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay
Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay
|
[PMID: 25970561] |
| Vero | EC50 |
1.5 μM
Compound: 12
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Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days
Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days
|
[PMID: 25970561] |
4α-Phorbol 12,13-didecanoate (10-50 μM) increases ATP release in urothelial cells[2].
4α-Phorbol 12,13-didecanoate (1-10 μM) increases Ca2+ in DRG neurons[3].
4α-Phorbol 12,13-didecanoate shows antiviral activities against CHIKV with an EC50 value of 1.5 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
4α-Phorbol 12,13-didecanoate (10-100 μM, intravesically administration) increases maximal micturition pressure in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:10, 25 and 100 μM
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Administration:Intravesically administration
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Result:Increased the amplitude of reflex bladder contractions.
Increase in the frequency of voiding.
Increased peak intravesical voiding pressures.
Chemical Information
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CAS No. 27536-56-7
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Appearance Solid-Liquid Mixture
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Molecular Weight 672.93
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Formula C40H64O8
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Color Colorless to off-white
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SMILES
CCCCCCCCCC(O[C@@]12[C@@]([C@@]3([H])[C@]([C@@H]([C@H]2OC(CCCCCCCCC)=O)C)([C@@]4([H])[C@@](CC(CO)=C3)(C(C(C)=C4)=O)O)O)([H])C1(C)C)=O
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Synonyms
4αPDD
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (148.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.72 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (809 KB)
- English - EN (809 KB)
- Français - FR (809 KB)
- Deutsch - DE (809 KB)
- Norwegian - NO (809 KB)
- Español - ES (809 KB)
- Swedish - SV (809 KB)
- Italian - IT (809 KB)
- Korean - KR (809 KB)
- Portuguese - PT (809 KB)
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Handling Instructions (2659 KB)
References
[1]. Hiromi Tsushima, et al. Antidipsogenic effects of a TRPV4 agonist, 4alpha-phorbol 12,13-didecanoate, injected into the cerebroventricle. Am J Physiol Regul Integr Comp Physiol. 2006 Jun;290(6):R1736-41. [Content Brief]
[2]. Lori Birder, et al. Activation of urothelial transient receptor potential vanilloid 4 by 4alpha-phorbol 12,13-didecanoate contributes to altered bladder reflexes in the rat. J Pharmacol Exp Ther. 2007 Oct;323(1):227-35. [Content Brief]
[3]. Alexander R, et al. 4α-phorbol 12,13-didecanoate activates cultured mouse dorsal root ganglia neurons independently of TRPV4. Br J Pharmacol. 2013 Feb;168(3):761-72. [Content Brief]
[4]. Nothias-Scaglia LF, et al. Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. J Nat Prod. 2015 Jun 26;78(6):1277-83. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4860 mL | 7.4302 mL | 14.8604 mL | 37.1510 mL |
| 5 mM | 0.2972 mL | 1.4860 mL | 2.9721 mL | 7.4302 mL | |
| 10 mM | 0.1486 mL | 0.7430 mL | 1.4860 mL | 3.7151 mL | |
| 15 mM | 0.0991 mL | 0.4953 mL | 0.9907 mL | 2.4767 mL | |
| 20 mM | 0.0743 mL | 0.3715 mL | 0.7430 mL | 1.8575 mL | |
| 25 mM | 0.0594 mL | 0.2972 mL | 0.5944 mL | 1.4860 mL | |
| 30 mM | 0.0495 mL | 0.2477 mL | 0.4953 mL | 1.2384 mL | |
| 40 mM | 0.0372 mL | 0.1858 mL | 0.3715 mL | 0.9288 mL | |
| 50 mM | 0.0297 mL | 0.1486 mL | 0.2972 mL | 0.7430 mL | |
| 60 mM | 0.0248 mL | 0.1238 mL | 0.2477 mL | 0.6192 mL | |
| 80 mM | 0.0186 mL | 0.0929 mL | 0.1858 mL | 0.4644 mL | |
| 100 mM | 0.0149 mL | 0.0743 mL | 0.1486 mL | 0.3715 mL |