YM-298198 hydrochloride
Based on 1 Customer Validation
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders.
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 1216398-09-2
- Formula: C18H23ClN4OS
- Molecular Weight:378.92
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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mGluR 1 |
YM-298198 hydrochloride shows a high affinity for mGluR1 with a Ki of 19 nM for rat mGluR1-NIH membranes[1].
YM-298198 hydrochloride inhibits glutamate-induced inositol phosphate production in mGluR1-NIH3T3 cells, with an IC50 of 16 nM[1].
YM-298198 hydrochloride shows neither agonistic nor antagonistic activity on mGluR2, 3, 4a, 6, or 7b up to 10 μM[1].
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 ICR mice[1]
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Dosage:30 mg/kg
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Administration:Oral administration
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Result:Prolonged nociceptive response latency in streptozotocin (200 mg/kg)-induced hyperalgesic mice.
Chemical Information
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CAS No. 1216398-09-2
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Appearance Solid
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Molecular Weight 378.92
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Formula C18H23ClN4OS
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Color White to light yellow
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SMILES
O=C(C1=C(C)N2C3=CC(N)=CC=C3N=C2S1)N(C4CCCCC4)C.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 125 mg/mL (329.88 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.08 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (274 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]. Kohara, A, et al. Radioligand Binding Properties and Pharmacological Characterization of 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a High-Affinity, Selective, and Noncompetitive Antagonist of Metabotropic Glutamate Receptor Type 1. J Pharmacol Exp Ther. 2005 Oct;315(1):163-9. [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 (sealed storage, away from moisture). 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 | 2.6391 mL | 13.1954 mL | 26.3908 mL | 65.9770 mL |
| 5 mM | 0.5278 mL | 2.6391 mL | 5.2782 mL | 13.1954 mL | |
| 10 mM | 0.2639 mL | 1.3195 mL | 2.6391 mL | 6.5977 mL | |
| 15 mM | 0.1759 mL | 0.8797 mL | 1.7594 mL | 4.3985 mL | |
| 20 mM | 0.1320 mL | 0.6598 mL | 1.3195 mL | 3.2988 mL | |
| 25 mM | 0.1056 mL | 0.5278 mL | 1.0556 mL | 2.6391 mL | |
| 30 mM | 0.0880 mL | 0.4398 mL | 0.8797 mL | 2.1992 mL | |
| 40 mM | 0.0660 mL | 0.3299 mL | 0.6598 mL | 1.6494 mL | |
| 50 mM | 0.0528 mL | 0.2639 mL | 0.5278 mL | 1.3195 mL | |
| 60 mM | 0.0440 mL | 0.2199 mL | 0.4398 mL | 1.0996 mL | |
| 80 mM | 0.0330 mL | 0.1649 mL | 0.3299 mL | 0.8247 mL | |
| 100 mM | 0.0264 mL | 0.1320 mL | 0.2639 mL | 0.6598 mL |
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