ML191
Based on 1 Customer Validation
ML191 (CID23612552) is a GPR55 antagonist. ML191 inhibits ERK phosphorylation and PKC β II translocation downstream of GPR55 signaling. ML191 suppresses LPI-induced activation of ERK1/2 and p38 MAPK signaling, blocks the transcription of RANKL-induced osteoclastogenesis markers, and reduces the bone resorption activity of mature osteoclasts promoted by RANKL. ML191 can be used to investigate diseases associated with bone degradation caused by excessive osteoclast activation, such as osteoporosis and bone damage during the formation stage of bone metastases.
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- Pureza: 99.81%
- No. CAS: 931695-79-3
- Fòrmula: C24H25N3O3
- Peso molecular:403.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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ERK1 |
ERK2 |
PKC-βII |
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Cell Line
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Type | Value | Description | References |
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| U2OS | IC50 |
1.1 μM
Compound: ML191; CID 23612552
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Antagonist activity at HA-epitope tagged GRP55E expressed with GFP-tagged beta-arr2 in human U2OS cells assessed as LPI-stimulated redistribution of beta-arr2 preincubated for 15 mins by beta-arrestin translocation assay
Antagonist activity at HA-epitope tagged GRP55E expressed with GFP-tagged beta-arr2 in human U2OS cells assessed as LPI-stimulated redistribution of beta-arr2 preincubated for 15 mins by beta-arrestin translocation assay
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[PMID: 26916440] |
ML191 (0.06-32 µM; 30-75 min) potently inhibits GPR55-mediated β-arrestin translocation in U2OS cells, with an IC50 of 1.08 µM. It exhibits over 29-fold selectivity over GPR35 and CB2, and only weak selectivity for the CB1 receptor[1].
ML191 (10-30 µM) inhibits GPR55-mediated PKCβII translocation in HEK293 cells, with the maximum inhibitory effect observed at 30 µM[1].
ML191 inhibits GPR55-mediated ERK1/2 phosphorylation in GPR55-expressing cells, with an EC50 of 0.143 µM[1].
ML191 (30 µM; 10 min pre-incubation, 10 min LPI stimulation) potently inhibits LPI-induced phosphorylation of ERK2 and p38 in shCTRL-HeLa cells, reducing the LPI-activated ERK2 level to 1.8-fold of the basal level and the p38 activation level to 1.2-fold of the basal level at 10 min post stimulation[2].
ML191 (0.5 µM; 72 h) inhibits RANKL-induced osteoclast maturation in RAW264.7 cells, reduces the mRNA levels of key osteoclastogenic markers (Nfatc1, Cathepsin-k, Mmp-9, Trap) by 30%-70%, and increases the mRNA level of Gpr55 to 46.1 times that of undifferentiated cells after 72 h of treatment[2].
ML191 (0.5 µM; 7 days) inhibits the bone resorption activity of mature osteoclasts differentiated from RAW264.7 cells, and reduces the total bone erosion area by 30% after 7 days of RANKL treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:shCTRL-HeLa
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Concentration:30 µM
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Incubation Time:10 min (pre-incubation); 5 min, 10 min (LPI stimulation)
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Result:Reduced LPI-stimulated ERK2 phosphorylation to 1.8-fold the ML191 basal level at 10 min of LPI stimulation.
Reduced LPI-stimulated p38 phosphorylation to 1.2-fold the ML191 basal level at 10 min of LPI stimulation.
Increased basal activation of both ERK2 and p38 significantly.
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Cell Line:RAW264.7
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Concentration:0.5 µM
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Incubation Time:72 h
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Result:Reduced Nfatc1 mRNA levels by 50% at 72 h.
Reduced Cathepsin-k mRNA levels by 60% at 72 h.
Reduced Mmp-9 mRNA levels by 30% at 72 h.
Reduced Trap mRNA levels by 70% at 72 h.
Caused no change in Ctr mRNA levels at 72 h.
Increased Gpr55 mRNA levels to 46.1-fold non-differentiated levels (1.8-fold relative to RANKL alone) at 72 h.
Chemical Information
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No. CAS 931695-79-3
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Appearance Solid
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Peso molecular 403.47
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Fòrmula C24H25N3O3
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Color Off-white to light yellow
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SMILES
O=C1OC(C2=CC=CC=C2)=NN1C3CCN(C(C4(C5=CC=C(C)C=C5)CC4)=O)CC3
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Synonyms
CID23612552
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (247.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Heynen-Genel S, et al. Screening for Selective Ligands for GPR55 - Antagonists. 2010 Oct 30 [updated 2011 May 26]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. [Content Brief]
[2]. Mosca MG, et al. Peptide targeting of lysophosphatidylinositol-sensing GPR55 for osteoclastogenesis tuning. Cell communication and signaling : CCS. 2021 Apr 26;19(1):48. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4785 mL | 12.3925 mL | 24.7850 mL | 61.9625 mL |
| 5 mM | 0.4957 mL | 2.4785 mL | 4.9570 mL | 12.3925 mL | |
| 10 mM | 0.2478 mL | 1.2392 mL | 2.4785 mL | 6.1962 mL | |
| 15 mM | 0.1652 mL | 0.8262 mL | 1.6523 mL | 4.1308 mL | |
| 20 mM | 0.1239 mL | 0.6196 mL | 1.2392 mL | 3.0981 mL | |
| 25 mM | 0.0991 mL | 0.4957 mL | 0.9914 mL | 2.4785 mL | |
| 30 mM | 0.0826 mL | 0.4131 mL | 0.8262 mL | 2.0654 mL | |
| 40 mM | 0.0620 mL | 0.3098 mL | 0.6196 mL | 1.5491 mL | |
| 50 mM | 0.0496 mL | 0.2478 mL | 0.4957 mL | 1.2392 mL | |
| 60 mM | 0.0413 mL | 0.2065 mL | 0.4131 mL | 1.0327 mL | |
| 80 mM | 0.0310 mL | 0.1549 mL | 0.3098 mL | 0.7745 mL | |
| 100 mM | 0.0248 mL | 0.1239 mL | 0.2478 mL | 0.6196 mL |
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