| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
EnMD-1068 (10 mM; 24 hours) reduces the release of calcium from HSCs induced by trypsin or SLIGRL-NH2. TGF-β1/Smad signaling is important for HSC activation and collagen synthesis. ENMD-1068 (10 mM) prevents this signaling in primary HSCs [1].
|
|---|---|
| ln Vivo |
Mice's liver fibrosis is inhibited by ENMD-1068 (25, 50 mg/kg; intraperitoneal injection; twice weekly for 4 weeks) [1]. One intraperitoneal injection of ENMD-1068 (25, 50 mg/kg) administered once daily for five days suppresses the proliferation of platelets controlled by endometriosis and dose-dependently lowers MCP-1 and IL-6 levels [2]. lasting five days) will cause mice's cell transplantation index to rise and their epithelial cell swelling to decrease [2].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Hepatic stellate cells (HSC) (stimulated by TGF-β1) Tested Concentrations: 10 mM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of TGF-β1-induced α-SMA, Col α1(І), Col Expression of α1(III) and Smad2/3 C-terminal phosphorylation. |
| Animal Protocol |
Animal/Disease Models: ICR mouse (8 weeks old; CCl4-induced liver fibrosis model) [1].
Doses: 25, 50 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a week for 4 weeks. Experimental Results: Collagen deposition was Dramatically weakened. Animal/Disease Models: Mice with surgically induced endometriosis [2]. Doses: 25, 50 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 5 days Experimental Results: Reduction in observed lesion volume in a dose-dependent manner. Inhibits the expression of IL-6 and MCP-1. Reduce the proliferation rate of endometriotic cells and increase 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
|
|---|---|
| Molecular Weight |
319.874
|
| CAS # |
789488-77-3
|
| Related CAS # |
ENMD-1068 hydrochloride;2703451-51-6;ENMD-1068 hydrobromide;644961-61-5
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
NCCCCCC(N1CCN(C(=O)CC(C)C)CC1)=O
|
| Synonyms |
ENMD 1068; ENMD-1068; ENMD1068
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
