ENMD-1068 hydrochloride
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.33%
- CAS No.: 2703451-51-6
- Formula: C15H30ClN3O2
- Molecular Weight:319.87
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ENMD-1068 hydrochloride
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Biological Activity
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PAR2 |
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.
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Cell Line:Hepatic stellate cells (HSCs) (TGF-β1-stimulated)
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Concentration:10 mM
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Incubation Time:24 h
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Result:Inhibited TGF-β1-induced expression of α-SMA, Col α1(І),Col α1(III), and Smad2/3 C-terminal phosphorylation.
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.
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Animal Model:ICR mice (8-week-old; CCl4-induced liver fibrosis model)[1].
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Dosage:25, 50 mg/kg
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Administration:Intraperitoneal injection; twice per week for 4 weeks
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Result:Markedly attenuated collagen deposition.
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Animal Model:Mice with surgically induced endometriosis[2].
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Dosage:25, 50 mg/kg
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Administration:Intraperitoneal injection; single daily for 5 days
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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.
Chemical Information
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CAS No. 2703451-51-6
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Appearance Solid
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Molecular Weight 319.87
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Formula C15H30ClN3O2
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Color White to off-white
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SMILES
O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Coagulation factor X promotes resistance to androgen-deprivation therapy in prostate cancer. [Abstract]2024 Oct 14;42(10):1676-1692.e11. PMID: 39303726 -
J Inflamm Res
Astragalus membranaceus and Salvia miltiorrhiza Inhibit Tryptase/PAR2-Mediated Mast Cells - Peritoneal Mesothelial Cells Crosstalk to Ameliorate Peritoneal Fibrosis. [Abstract]2026 May 11:19:577472. PMID: 42147796 -
Solvent & Solubility
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)
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.
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.
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: 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.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (312.63 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Sun Q, et al. ENMD-1068 inhibits liver fibrosis through attenuation of TGF-β1/Smad2/3 signaling in mice. Sci Rep. 2017 Jul 14;7(1):5498. doi: 10.1038/s41598-017-05190-7. Erratum in: Sci Rep. 2019 Dec 10;9(1):19125. [Content Brief]
[2]. Wang Y, et al. ENMD-1068, a protease-activated receptor 2 antagonist, inhibits the development of endometriosis in a mouse model. Am J Obstet Gynecol. 2014 Jun;210(6):531.e1-8. [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 (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.
ENMD-1068 hydrochloride Related Classifications
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