| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
PAR2
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|---|---|
| ln Vitro |
In primary mouse HSCs, ENMD-1068 (10 mM; 24 h) inhibits TGF-β1/Smad signaling (the TGF-β1/Smad signal pathway is essential for HSC activation and collagen production)[1]. Inhibiting trypsin or SLIGRL-NH2 induced calcium release in HSCs is the effect of ENMD-1068 (10 mM; 24 h)[1].
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| ln Vivo |
ENMD-1068 (i.p.; 25–50 mg/kg; twice weekly for 4 weeks) prevents mice's liver fibrosis[1]. In a dose-dependent way, ENMD-1068 (25, 50 mg/kg; ip; once daily for 5 days) reduces the progression of endometriosis and decreases the levels of IL-6 and MCP-1[2]. In mice, ENMD-1068 (25, 50 mg/kg; ip; once daily for 5 days) reduces the proliferation of epithelial cells and raises the apoptotic index[2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Hepatic stellate cells (HSCs) (TGF-β1-stimulated) Tested Concentrations: 10 mM Incubation Duration: 24 h Experimental Results: Inhibited TGF-β1-induced expression of α-SMA, Col α1(І),Col α1(III), and Smad2/ 3 C-terminal phosphorylation. |
| Animal Protocol |
Animal/Disease Models: ICR mice (8weeks old; CCl4-induced liver fibrosis model)[1].
Doses: 25, 50 mg/kg Route of Administration: intraperitoneal (ip)injection; twice per week for 4 weeks Experimental Results: Markedly attenuated collagen deposition. Animal/Disease Models: Mice with surgically induced endometriosis[2]. Doses: 25, 50 mg/kg Route of Administration: intraperitoneal (ip)injection; single daily for 5 days Experimental Results: diminished the volume of observed lesions in a dose-dependent manner. Inhibited the expression of IL-6 and MCP-1. diminished the proliferation rate of endometriotic cells and increased the percentage of apoptotic epithelial cells in the lesions. |
| 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.
[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. |
| Molecular Formula |
C15H30CLN3O2
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|---|---|
| Molecular Weight |
319.87
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| CAS # |
2703451-51-6
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| Related CAS # |
ENMD-1068 hydrobromide;644961-61-5;ENMD-1068;789488-77-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
Cl.O=C(CCCCCN)N1CCN(C(CC(C)C)=O)CC1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 200 mg/mL (625.25 mM)
H2O : 100 mg/mL (312.63 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (15.63 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (15.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (15.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (312.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3126 mL | 1.5631 mL | 3.1263 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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