YM 90K hydrochlorideCAS# 154164-30-4 |
- YM155
Catalog No.:BCC2251
CAS No.:781661-94-7
Quality Control & MSDS
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| Cas No. | 154164-30-4 | SDF | Download SDF |
| PubChem ID | 5486547 | Appearance | Powder |
| Formula | C11H8ClN5O4 | M.Wt | 309.67 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in DMSO with gentle warming | ||
| Chemical Name | 6-imidazol-1-yl-7-nitro-1,4-dihydroquinoxaline-2,3-dione;hydrochloride | ||
| SMILES | C1=CN(C=N1)C2=C(C=C3C(=C2)NC(=O)C(=O)N3)[N+](=O)[O-].Cl | ||
| Standard InChIKey | UMLFDVOHVJPDIZ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H7N5O4.ClH/c17-10-11(18)14-7-4-9(16(19)20)8(3-6(7)13-10)15-2-1-12-5-15;/h1-5H,(H,13,17)(H,14,18);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 | Selective AMPA receptor antagonist (Ki values are 84, 2200 and > 37000 nM for AMPA, kainate and NMDA receptors respectively). Neuroprotective; delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration. |
YM 90K hydrochloride Dilution Calculator
YM 90K hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2292 mL | 16.1462 mL | 32.2924 mL | 64.5849 mL | 80.7311 mL |
| 5 mM | 0.6458 mL | 3.2292 mL | 6.4585 mL | 12.917 mL | 16.1462 mL |
| 10 mM | 0.3229 mL | 1.6146 mL | 3.2292 mL | 6.4585 mL | 8.0731 mL |
| 50 mM | 0.0646 mL | 0.3229 mL | 0.6458 mL | 1.2917 mL | 1.6146 mL |
| 100 mM | 0.0323 mL | 0.1615 mL | 0.3229 mL | 0.6458 mL | 0.8073 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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A potent AMPA/kainate receptor antagonist, YM90K, attenuates the loss of N-acetylaspartate in the hippocampal CA1 area after transient unilateral forebrain ischemia in gerbils.[Pubmed:11589513]
Life Sci. 2001 Sep 14;69(17):1983-90.
By analyzing histological damages and the regional N-acetylaspartate (NAA) level simultaneously, we evaluated the effect of an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA)/kainate receptor antagonist, YM90K [6-(1H-imidazol-1-yl)-7-nitro-2,3-(1H,4H)-quinoxalinedione monohydrochloride], in unilateral forebrain ischemia in gerbils. The right common carotid artery was clipped for 5 min under ether anesthesia, and reperfused for 7 days. The frozen brain sections were lyophilized and the hippocampal CA1 area was dissected out for HPLC assay of NAA. An adjacent section was stained with hematoxylin-eosin for counting survived neurons per 1 mm pyramidal layer of the hippocampal CA1 area. Postischemic administration of YM90K at 20 mg/kg and 25 mg/kg attenuated the decrease of both the number of survived neurons and the NAA level on the ischemic side in a dose-dependent manner. A significant linear correlation was observed between the NAA level and the number of intact neurons. These results indicated that the NAA level could be used as an index of neuroprotective effects of pharmacological agents in global cerebral ischemia.
Neuroprotective effect of a novel AMPA receptor antagonist, YM90K, in rat focal cerebral ischaemia.[Pubmed:9409705]
Brain Res. 1997 Oct 31;773(1-2):61-5.
It has been reported that delayed treatment with alpha-amino-3-hydroxy-5-methyl-4-isoxazole (AMPA) receptor antagonists was able to more completely inhibit glutamate neurotoxicity than N-methyl-D-aspartate (NMDA) receptor antagonists. Therefore, we investigated the neuroprotective effect of YM90K, an AMPA receptor antagonist, on focal cerebral lesions induced by thrombotic middle cerebral artery (MCA) occlusion in rats, particularly in the early phase of the cerebral ischaemic lesions. The MCA was occluded by photochemical reaction between transmural green light and systemically administered Rose Bengal, which causes endothelial injury followed by platelet adhesion, aggregation and formation of a platelet and fibrin-rich thrombus at the site of photochemical reaction. The infarct size was measured at 24 and 72 h after the MCA occlusion by a histochemical technique. YM90K was administered at various doses as a continuous infusion for 4 h, beginning 0 to 3 h after the MCA occlusion. YM90K (10 and 20 mg/kg per h for 4 h continuous infusion), starting immediately after the MCA occlusion significantly (P < 0.05) reduced the infarct size at 24 h after MCA occlusion in a dose-dependent manner. Further, the agent showed the same efficacy at 72 h after. The inhibitory effect of YM90K (20 mg/kg per h) on the infarct size was the same when the drug was started immediately, 1, 2 and 3 h after MCA occlusion. In conclusion, the novel AMPA receptor antagonist YM90K was effective in the treatment of focal cerebral ischaemic lesions. Activation of AMPA receptor may play a key role in the development of cerebral infarct in the early phase of ischaemia in rats.
6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: structure-activity relationships for the AMPA-type non-NMDA receptor.[Pubmed:8120865]
J Med Chem. 1994 Feb 18;37(4):467-75.
A novel series of quinoxalinediones possessing imidazolyl and related heteroaromatic substituents was synthesized and evaluated for their activity to inhibit [3H]AMPA binding from rat whole brain. From the structure-activity relationships, it was found that the 1H-imidazol-1-yl moiety could function as a bioisostere for the cyano and nitro groups, and that 6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione (11) showed the most potent activity for the AMPA receptor. Compound 11 was evaluated for selectivity versus other excitatory amino acid receptors, and its action against AMPA at its receptor in the rat striatum was characterized. These data showed that compound 11 was a selective antagonist for the AMPA receptor with a Ki value of 0.084 microM, being approximately equipotent with 2,3-dihydro-6-nitro-7-sulfamoylbenzo(f)quinoxaline (3) (NBQX; Ki = 0.060 microM). Compound 11 was also found to give protection against sound-induced seizure on DBA/2 mice at the minimum effective dose of 3 mg/kg ip (3; 10 mg/kg ip).
