2. Metabolic Enzyme/Protease
  3. Phosphatase Dopamine β-hydroxylase
  4. EWP 815

EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity.

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EWP 815 Chemical Structure

EWP 815 Chemical Structure

CAS No. : 20231-01-0

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Based on 1 publication(s) in Google Scholar

EWP 815 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity[1][2].

IC50 & Target

Ins(1,4)P2 phosphatase; Ins(1,4,5)P3 5-phosphatase[1]; dopamine β-hydroxylase[2]
In Vitro

EWP 815 inhibits thyrotropin-releasing hormone (TRH; 0.03 mM)-stimulated inositol phospholipid breakdown without affecting basal breakdown rates in prelabelled GH3 cells with IC50s of 83 mM (soluble enzymes) and 71 mM (particulate enzymes), respectively[1].
EWP 815 (30 μM; 1 h) exerts higher inhibition on Ins(1,4)P2 phosphatase rather than Ins(1,4,5)P3 5-phosphatase with the mean [3H]Ins(1,4)P2/mean [3H]InsP recovery ratio of 2.6[1].
EWP 815 (6, 8 μM; 10 min) inhibits dephosphorylation of [3H]Ins(1,4,5)P3 5-phosphatase in particulate and soluble fractions with IC50s of 6 μM and 8 μM, respectively[1].
EWP 815 (3-300 μM; 30 min) suppresses thyrotropin-releasing hormone (TRH)-stimulated (100 nM) inositol phospholipid production by 30% (100 μM) and 1.8% (300 μM), respectively, without affecting Ins(1,4,5)P3 binding[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EWP 815 Related Antibodies
In Vivo

EWP 815 (50 mg/kg; i.p.; 30 min before killed) inhibits the enzyme dopamine β-hydroxylase activity in mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female mice (20 g)[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 30 min before killed
Result: Intraperitoneal injection; 30 min before killedInhibited β-hydroxylase of 3H-α-methyldopamine.
Reduced the amount of 3H-α-Me-NA by 12%.
Molecular Weight

350.59

Formula

C12H22N4S4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

S=C(N1CCN(C)CC1)SSC(N2CCN(C)CC2)=S
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (142.62 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 2.8523 mL 14.2617 mL 28.5233 mL
5 mM 0.5705 mL 2.8523 mL 5.7047 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 (protect from light). 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (3.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 1.25 mg/mL (3.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). 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 (12.5 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.
Purity & Documentation
References

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 (protect from light). 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 2.8523 mL 14.2617 mL 28.5233 mL 71.3084 mL
5 mM 0.5705 mL 2.8523 mL 5.7047 mL 14.2617 mL
10 mM 0.2852 mL 1.4262 mL 2.8523 mL 7.1308 mL
15 mM 0.1902 mL 0.9508 mL 1.9016 mL 4.7539 mL
20 mM 0.1426 mL 0.7131 mL 1.4262 mL 3.5654 mL
25 mM 0.1141 mL 0.5705 mL 1.1409 mL 2.8523 mL
30 mM 0.0951 mL 0.4754 mL 0.9508 mL 2.3769 mL
40 mM 0.0713 mL 0.3565 mL 0.7131 mL 1.7827 mL
50 mM 0.0570 mL 0.2852 mL 0.5705 mL 1.4262 mL
60 mM 0.0475 mL 0.2377 mL 0.4754 mL 1.1885 mL
80 mM 0.0357 mL 0.1783 mL 0.3565 mL 0.8914 mL
100 mM 0.0285 mL 0.1426 mL 0.2852 mL 0.7131 mL
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EWP 815 Related Classifications

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.

Keywords:

EWP 81520231-01-0EWP815EWP-815PhosphataseDopamine β-hydroxylaseDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenasea-methyldopammeprotrlptyhnedopamme β-hydroxylasereserpinestereospeelficlty malamldeInhibitorinhibitorinhibit

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