1. Membrane Transporter/Ion Channel Neuronal Signaling Anti-infection
  2. TRP Channel CHIKV
  3. 4α-Phorbol 12,13-didecanoate

4α-Phorbol 12,13-didecanoate  (Synonyms: 12,13-ジデカン酸4α-ホルボール)

製品番号: HY-116291 純度: 99%
COA 取扱説明書 Technical Support

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).

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4α-Phorbol 12,13-didecanoate

4α-Phorbol 12,13-didecanoate 構造式

CAS 番号 : 27536-56-7

容量 価格(税別) 在庫状況 数量
1 mg $930 在庫あり
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10 mg   お問い合わせ  

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製品説明

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)[1][2][3][4].

IC50 & Target[1]

TRPV4

 

Cellular Effect
Cell Line Type Value Description References
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
[PMID: 19361196]
HEK293 EC50
0.37 μM
Compound: 2a, 4alpha-PDD
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
[PMID: 19361196]
HEK293 EC50
6.3 μM
Compound: 2a, 4alpha-PDD
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]
HEK293 EC50
> 6 μM
Compound: 2a, 4alpha-PDD
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
[PMID: 19361196]
MT4 EC50
> 16 μM
Compound: 12
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
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
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]
体外実験

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.

体内実験

4α-Phorbol 12,13-didecanoate (20 μg, intracerebroventricular injection) inhibits water intake in WT rats[1].
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.

Animal Model: Rats[1]
Dosage: 10, 25 and 100 μM
Administration: Intravesically administration
Result: Increased the amplitude of reflex bladder contractions.
Increase in the frequency of voiding.
Increased peak intravesical voiding pressures.
分子量

672.93

分子式

C40H64O8

CAS 番号
Appearance

Solid-Liquid Mixture

Color

Colorless to off-white

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Pure form -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4860 mL 7.4302 mL 14.8604 mL
5 mM 0.2972 mL 1.4860 mL 2.9721 mL
10 mM 0.1486 mL 0.7430 mL 1.4860 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (3.72 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.30%

参考文献

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
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
4α-Phorbol 12,13-didecanoate
製品番号:
HY-116291
数量:
MCE 日本正規代理店: