Desmethyl-YM 298198CAS# 1177767-57-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1177767-57-5 | SDF | Download SDF |
PubChem ID | 16759180 | Appearance | Powder |
Formula | C17H21ClN4OS | M.Wt | 364.89 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 50 mM in DMSO | ||
Chemical Name | 7-amino-N-cyclohexyl-1-methyl-[1,3]thiazolo[3,2-a]benzimidazole-2-carboxamide;hydrochloride | ||
SMILES | CC1=C(SC2=NC3=C(N12)C=C(C=C3)N)C(=O)NC4CCCCC4.Cl | ||
Standard InChIKey | SWKZWXJQIDXGLX-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C17H20N4OS.ClH/c1-10-15(16(22)19-12-5-3-2-4-6-12)23-17-20-13-8-7-11(18)9-14(13)21(10)17;/h7-9,12H,2-6,18H2,1H3,(H,19,22);1H | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Derivative of the mGlu1-selective antagonist YM 298198. |
Desmethyl-YM 298198 Dilution Calculator
Desmethyl-YM 298198 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.7406 mL | 13.7028 mL | 27.4055 mL | 54.811 mL | 68.5138 mL |
5 mM | 0.5481 mL | 2.7406 mL | 5.4811 mL | 10.9622 mL | 13.7028 mL |
10 mM | 0.2741 mL | 1.3703 mL | 2.7406 mL | 5.4811 mL | 6.8514 mL |
50 mM | 0.0548 mL | 0.2741 mL | 0.5481 mL | 1.0962 mL | 1.3703 mL |
100 mM | 0.0274 mL | 0.137 mL | 0.2741 mL | 0.5481 mL | 0.6851 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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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.[Pubmed:15976016]
J Pharmacol Exp Ther. 2005 Oct;315(1):163-9.
Metabotropic glutamate receptor type 1 (mGluR1) is thought to play important roles in the neurotransmission and pathogenesis of several neurological disorders. Here, we describe the radioligand binding properties and pharmacological effects of a newly synthesized, high-affinity, selective, and noncompetitive mGluR1 antagonist, 6-amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198). YM-298198 inhibited glutamate-induced inositol phosphate production in mGluR1-NIH3T3 cells with an IC50 of 16 +/- 5.8 nM in a noncompetitive manner. Its radiolabeled form, [3H]YM-298198, bound to mGluR1-NIH3T3 cell membranes with a KD of 32 +/- 8.5 nM and a Bmax of 2297 +/- 291 fmol/mg protein. In ligand displacement experiments using rat cerebellum membrane, an existing noncompetitive mGluR1 antagonist 7-(hydroxyimino)cyclo-propa[b]chromen-1a-carboxylate ethyl ester (CPCCOEt) competitively displaced [3H]YM-298198 binding, although glutamate and other mGluR1 ligands acting on a glutamate site failed to inhibit [3H]YM-298198 binding, suggesting that YM-298198 binds to CPCCOEt (allosteric) binding sites but not to glutamate (agonist) binding sites. Specificity was demonstrated for mGluR1 over mGluR subtypes 2 to 7, ionotropic glutamate receptors, and other receptor, transporter, and ion channel targets. In in vivo experiments, orally administered YM-298198 showed a significant analgesic effect in streptozotocin-induced hyperalgesic mice at doses (30 mg/kg) that did not cause Rotarod performance impairment, indicating that it is also useful even for in vivo experiments. In conclusion, YM-298198 is a newly synthesized, high-affinity, selective, and noncompetitive antagonist of mGluR1 that will be a useful pharmacological tool due to its highly active properties in vitro and in vivo. Its radiolabeled form [3H]YM-298198 will also be a valuable tool for future investigation of the mGluR1.
Potent and specific action of the mGlu1 antagonists YM-298198 and JNJ16259685 on synaptic transmission in rat cerebellar slices.[Pubmed:17502847]
Br J Pharmacol. 2007 Jul;151(6):870-6.
BACKGROUND AND PURPOSE: Specific and selective inhibitors for mGlu1 receptors are presently inadequate. A new generation of non-competitive mGlu1 antagonists with low nanomolar potencies is emerging. We evaluated two new compounds, YM-298198 and JNJ16259685, for effectiveness, potency and specificity for the first time in a brain slice preparation. EXPERIMENTAL APPROACH: Patch-clamp recording of Purkinje neurones in cerebellar slices were obtained. The slow mGlu1-mediated EPSP was used to establish a concentration-response curve. Fast excitatory synaptic inputs were tested for non-specific effects. KEY RESULTS: YM-298198 and JNJ16259685 inhibited the synaptic activation of mGlu1 in a concentration-dependent manner (IC(50) values of 24 nM and 19 nM, respectively). The antagonists were slow to inhibit and to reverse on washout, probably due to their lipophilic nature. There were no non-specific effects on fast AMPA receptor-mediated synaptic transmission in the cerebellum. CONCLUSIONS AND IMPLICATIONS: These compounds are more than a thousand-fold more potent than previously available compounds. Their selectivity and specificity will be very useful for studying the role of mGlu1 receptors both in vitro and in vivo.