1. GPCR/G Protein Apoptosis
  2. Protease Activated Receptor (PAR) Apoptosis
  3. ENMD-1068 hydrochloride

ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.

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ENMD-1068 hydrochloride Chemical Structure

ENMD-1068 hydrochloride Chemical Structure

CAS No. : 2703451-51-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 170 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ENMD-1068 hydrochloride:

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1 Publications Citing Use of MCE ENMD-1068 hydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis[1][2].

IC50 & Target

PAR2

 

In Vitro

ENMD-1068 (10 mM; 24 h) blocks TGF-β1/Smad signaling in primary mouse HSCs (TGF-β1/Smad signal pathway plays a crucial role in HSCs activation and collagen production)[1].
ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs[1].

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

Western Blot Analysis[1]

Cell Line: Hepatic stellate cells (HSCs) (TGF-β1-stimulated)
Concentration: 10 mM
Incubation Time: 24 h
Result: Inhibited TGF-β1-induced expression of α-SMA, Col α1(І),Col α1(III), and Smad2/3 C-terminal phosphorylation.
In Vivo

ENMD-1068 (25, 50 mg/kg; i.p.; twice per week for 4 weeks) inhibits liver fibrosis of mice[1].
ENMD-1068 (25, 50 mg/kg; i.p.; single daily for 5 days) inhibits endometriosis growth and suppresses the levels of IL-6 and MCP-1 in a dose-dependent manner[2].
ENMD-1068 (25, 50 mg/kg; i.p.; single daily for 5 days) causes a decrease in epithelial cell proliferation and an increase in the apoptotic index in mice[2].

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

Animal Model: ICR mice (8-week-old; CCl4-induced liver fibrosis model)[1].
Dosage: 25, 50 mg/kg
Administration: Intraperitoneal injection; twice per week for 4 weeks
Result: Markedly attenuated collagen deposition.
Animal Model: Mice with surgically induced endometriosis[2].
Dosage: 25, 50 mg/kg
Administration: Intraperitoneal injection; single daily for 5 days
Result: Reduced the volume of observed lesions in a dose-dependent manner.
Inhibited the expression of IL-6 and MCP-1.
Decreased the proliferation rate of endometriotic cells and increased the percentage of apoptotic epithelial cells in the lesions.
Molecular Weight

319.87

Formula

C15H30ClN3O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (625.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (312.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1263 mL 15.6314 mL 31.2627 mL
5 mM 0.6253 mL 3.1263 mL 6.2525 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 5 mg/mL (15.63 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (312.63 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 (stored under nitrogen). 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
H2O / DMSO 1 mM 3.1263 mL 15.6314 mL 31.2627 mL 78.1568 mL
5 mM 0.6253 mL 3.1263 mL 6.2525 mL 15.6314 mL
10 mM 0.3126 mL 1.5631 mL 3.1263 mL 7.8157 mL
15 mM 0.2084 mL 1.0421 mL 2.0842 mL 5.2105 mL
20 mM 0.1563 mL 0.7816 mL 1.5631 mL 3.9078 mL
25 mM 0.1251 mL 0.6253 mL 1.2505 mL 3.1263 mL
30 mM 0.1042 mL 0.5210 mL 1.0421 mL 2.6052 mL
40 mM 0.0782 mL 0.3908 mL 0.7816 mL 1.9539 mL
50 mM 0.0625 mL 0.3126 mL 0.6253 mL 1.5631 mL
60 mM 0.0521 mL 0.2605 mL 0.5210 mL 1.3026 mL
80 mM 0.0391 mL 0.1954 mL 0.3908 mL 0.9770 mL
100 mM 0.0313 mL 0.1563 mL 0.3126 mL 0.7816 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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ENMD-1068 hydrochloride Related Classifications

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  • 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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ENMD-1068 hydrochloride
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