ML-193
Based on 2 publication(s) in Google Scholar
ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.
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- Purity: 99.68%
- CAS No.: 713121-80-3
- 화학식: C28H25N5O4S
- 분자량:527.59
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Anti-Parkinson's Disease Compound Library
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Publications Citing Use of MedChemExpress (MCE) ML-193
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Biological Activity
IC50: 221 nM (GPR55)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2OS | IC50 |
0.22 μM
Compound: ML193
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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] |
ML-193 (0.01-100 μM; pretreated for 15 min) inhibits β-arrestin trafficking induced by L-α-lysophophosphatidylinositol (LPI, 10 μM) and ML186 (1 μM) with IC50s of 0.22 μM and 0.12 μM, respectively[2].
ML-193 (0.01-10 μM; pretreated for 30 min) decreases the LPI-mediated ERK1/2 phosphorylation, with an IC50 of 0.2 μM in U2OS cells[2].
ML-193 (5 μM; pretreated for 30 min) attenuates the GPR55 agonists induced increases in hNSCs proliferation rates[4].
ML-193 (5 μM; 10 d) attenuates the ML184-induced increases in hNSCs differentiation[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (200-250 g) were induced experimental Parkinson by 6-hydroxydopamine (6-OHDA, 10 µg/rat)[3]
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Dosage:1 and 5 µg/rat
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Administration:Injected into the right striatum at a rate of 1 μL/min
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Result:Increased the time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats.
Chemical Information
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CAS No. 713121-80-3
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Appearance Solid
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분자량 527.59
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화학식 C28H25N5O4S
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Color White to light yellow
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SMILES
CC(C(C)=NO1)=C1NS(C(C=C2)=CC=C2NC(C3=CC(C4=CC=CC=N4)=NC5=C3C=C(C)C=C5C)=O)(=O)=O
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Synonyms
CID 1261822
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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EMBO J
Hepatic ASPG-mediated lysophosphatidylinositol catabolism impairs insulin signal transduction. [Abstract]2025 Aug 4. PMID: 40760121 -
Sci Rep
Activating GPR55 protects cochlear hair cells against cisplatin-induced ototoxicity via inhibiting MAPK pathway. [Abstract]2026 Apr 14;16(1):17287. PMID: 41981055
용액&용해도
DMSO : 100 mg/mL (189.54 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.74 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Heynen-Genel S, et, al. Screening for Selective Ligands for GPR55-Antagonists. Probe Reports from the NIH Molecular Libraries Program. 2010 Oct 30. [Content Brief]
[2]. Kotsikorou E, et, al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2013 Dec 31;52(52):9456-69. [Content Brief]
[3]. Fatemi I, et, al. The effect of intra-striatal administration of GPR55 agonist (LPI) and antagonist (ML193) on sensorimotor and motor functions in a Parkinson's disease rat model. Acta Neuropsychiatr. 2021 Feb;33(1):15-21. [Content Brief]
[4]. Hill JD, et, al. Activation of GPR55 increases neural stem cell proliferation and promotes early adult hippocampal neurogenesis. Br J Pharmacol. 2018 Aug;175(16):3407-3421. [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 | 1.8954 mL | 9.4771 mL | 18.9541 mL | 47.3853 mL |
| 5 mM | 0.3791 mL | 1.8954 mL | 3.7908 mL | 9.4771 mL | |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8954 mL | 4.7385 mL | |
| 15 mM | 0.1264 mL | 0.6318 mL | 1.2636 mL | 3.1590 mL | |
| 20 mM | 0.0948 mL | 0.4739 mL | 0.9477 mL | 2.3693 mL | |
| 25 mM | 0.0758 mL | 0.3791 mL | 0.7582 mL | 1.8954 mL | |
| 30 mM | 0.0632 mL | 0.3159 mL | 0.6318 mL | 1.5795 mL | |
| 40 mM | 0.0474 mL | 0.2369 mL | 0.4739 mL | 1.1846 mL | |
| 50 mM | 0.0379 mL | 0.1895 mL | 0.3791 mL | 0.9477 mL | |
| 60 mM | 0.0316 mL | 0.1580 mL | 0.3159 mL | 0.7898 mL | |
| 80 mM | 0.0237 mL | 0.1185 mL | 0.2369 mL | 0.5923 mL | |
| 100 mM | 0.0190 mL | 0.0948 mL | 0.1895 mL | 0.4739 mL |
ML-193 Related Classifications
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