FTIDC |
Catalog No.GC50087
One-Click Copy Product Info
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Potent and selective negative allosteric modulator of mGlu1 receptors; also mGlu1 inverse agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 873551-53-2
Sample solution is provided at 25 µL, 10mM.
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Potent and selective mGlu1 receptor negative allosteric modulator (IC50 values are 5.8 and 6200 nM for mGlu1 and mGlu5 respectively). Also acts as an mGlu1 receptor inverse agonist (IC50 = 7 nM) in the absence of ligand. Exhibits no effect at group II/III mGlu receptors. Inhibits L-glutamate-induced increases in intracellular calcium in mGlu1-expressing CHO cells. Inhibits nociceptive behavior, and exhibits anxiolytic and antipsychotic effects in vivo. Orally active.
Suzuki et al (2007) Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1( J.Pharmacol.Exp.Ther. 321 1144 PMID:17360958 |Ito et al (2008) Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist. Bioorg.Med.Chem. 16 9817 PMID:18849168 |Satow et al (2008) Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allost J.Pharmacol.Exp.Ther. 326 577 PMID:18487514
| Cas No. | 873551-53-2 | SDF | |
| Canonical SMILES | O=C(N(C(C)C)C)N1CC=C(C2=C(C)N(C3=C(F)N=CC=C3)N=N2)CC1 | ||
| Formula | C18H23FN6O | M.Wt | 358.41 |
| Solubility | DMSO : ≥ 100 mg/mL (279.01 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7901 mL | 13.9505 mL | 27.901 mL |
| 5 mM | 558 μL | 2.7901 mL | 5.5802 mL |
| 10 mM | 279 μL | 1.3951 mL | 2.7901 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)