| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| ln Vitro |
ML-180 (SR1848; 0.01-100 µM; 48 hours) exhibits decreased proliferation in Huh-7 cells at concentrations greater than 1 µM, with an EC50 of roughly 2.8 µM. In an LRH-1-dependent manner, ML-180 suppresses cell growth [2]. Although ML-180 (0.5–5 µM; 24 hours) has minimal effect on the inhibition in SK-OV-3 cells, it significantly inhibits the expression of cyclin-D1 and cyclin-E1 in hepatocytes [2]. LRH-1 expression is rapidly reduced and endogenous LRH-1 signaling is efficiently inhibited by ML-180 (5 µM; 24 hours) [2]. LRH-1 mRNA expression is dose-dependently inhibited by ML-180 (0.5–5 µM; 24 hours) [2]. In Huh-7 and HepG2 cells, ML-180 (5 μM; 2 hours) immediately and dramatically lowers the mRNA levels of the LRH-1 receptor and its downstream targets (CYP19, GATA3, and GATA4) [2].
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| ln Vivo |
In adrenal and pancreatic tissues, ML-180 (SR1848; 30 mg/kg; i.p.; daily; for 10 days) resulted in a statistically significant reduction in LRH-1 and SHP mRNA [2].
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| Cell Assay |
Cell proliferation assay [2]
Cell Types: Huh-7 Cell Tested Concentrations: 0.01, 0.1, 1, 10, 100 µM Incubation Duration: 48 hrs (hours) Experimental Results: Proliferation ability is diminished at concentrations higher than 1 µM. Cell cycle analysis [2] Cell Types: Huh-7 Cell Tested Concentrations: 0.5, 1, 5 µM Incubation Duration: 24 hrs (hours) Experimental Results: Significant inhibitory effect on the expression of cyclin-D1 and cyclin-E1 in hepatocytes. Western Blot Analysis[2] Cell Types: Huh-7 Cell Tested Concentrations: 5 µM Incubation Duration: 24 hrs (hours) Experimental Results: LRH-1 protein levels were Dramatically diminished. RT-PCR[2] Cell Types: Huh-7 Cell Tested Concentrations: 0.5, 1, 5 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of LRH-1 mRNA expression in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: 8weeks old C57Bl/6J mice [2]
Doses: 30 mg/kg Route of Administration: IP; daily; lasted for 10 days Experimental Results: LRH-1 and SHP mRNA in adrenal gland and pancreatic tissue demonstrated statistically significant levels falling. |
| References | |
| Additional Infomation |
6-[4-(3-chlorophenyl)-1-piperazinyl]-3-cyclohexyl-1H-pyrimidine-2,4-dione is a member of piperazines.
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| Molecular Formula |
C₂₀H₂₅CLN₄O₂
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|---|---|
| Molecular Weight |
388.89
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| Exact Mass |
388.166
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| CAS # |
863588-32-3
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| PubChem CID |
3238389
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.619
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| LogP |
4.43
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
597
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CHMQQIFPOIZPIJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25ClN4O2/c21-15-5-4-8-17(13-15)23-9-11-24(12-10-23)18-14-19(26)25(20(27)22-18)16-6-2-1-3-7-16/h4-5,8,13-14,16H,1-3,6-7,9-12H2,(H,22,27)
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| Chemical Name |
6-[4-(3-chlorophenyl)piperazin-1-yl]-3-cyclohexyl-1H-pyrimidine-2,4-dione
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| Synonyms |
ML180; ML 180
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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 : ~11.9 mg/mL (~30.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.19 mg/mL (3.06 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 11.9 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. Solubility in Formulation 2: ≥ 1.19 mg/mL (3.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 11.9 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2 mg/mL (5.14 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL | |
| 5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL | |
| 10 mM | 0.2571 mL | 1.2857 mL | 2.5714 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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