U 90042GABAA receptor ligand CAS# 134516-99-7 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 134516-99-7 | SDF | Download SDF |
| PubChem ID | 9928470 | Appearance | Powder |
| Formula | C17H13ClN6O | M.Wt | 352.78 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 30 mM in DMSO and to 5 mM in ethanol | ||
| SMILES | C1CC1C2=NC(=NO2)C3=C4N5CCN=C5C6=C(N4C=N3)C=CC(=C6)Cl | ||
| Standard InChIKey | CLPSAAPUJUVQPP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H13ClN6O/c18-10-3-4-12-11(7-10)15-19-5-6-23(15)17-13(20-8-24(12)17)14-21-16(25-22-14)9-1-2-9/h3-4,7-9H,1-2,5-6H2 | ||
| 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 | GABAA receptor ligand that binds with comparable affinities to three receptor subtypes: α1β2γ2, α3β2γ2 and α6β2γ2 (Ki values are 7.8, 9.5 and 11.0 nM respectively). Potentiates GABA-induced chloride currents in α6β2γ2 receptors. Sedative/hypnotic compound. |
U 90042 Dilution Calculator
U 90042 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8346 mL | 14.1731 mL | 28.3463 mL | 56.6926 mL | 70.8657 mL |
| 5 mM | 0.5669 mL | 2.8346 mL | 5.6693 mL | 11.3385 mL | 14.1731 mL |
| 10 mM | 0.2835 mL | 1.4173 mL | 2.8346 mL | 5.6693 mL | 7.0866 mL |
| 50 mM | 0.0567 mL | 0.2835 mL | 0.5669 mL | 1.1339 mL | 1.4173 mL |
| 100 mM | 0.0283 mL | 0.1417 mL | 0.2835 mL | 0.5669 mL | 0.7087 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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U-90042, a sedative/hypnotic compound that interacts differentially with the GABAA receptor subtypes.[Pubmed:7473164]
J Pharmacol Exp Ther. 1995 Nov;275(2):761-7.
U-90042 is a structurally novel compound that has comparable affinities for binding to three recombinant subtypes of the gamma-aminobutyric acidA receptor: alpha 1 beta 2 gamma 2, alpha 3 beta 2 gamma 2 and alpha 6 beta 2 gamma 2. The relatively high affinity for the alpha 6 beta 2 gamma 2 subtype is similar to the benzodiazepine (BZ) partial inverse agonist Ro 15-4513 and different from BZ sedative/hypnotics such as diazepam and zolpidem. In the present study, U-90042 (3 mg/kg i.p.) suppressed locomotor activity and impaired rotarod performance in mice. These effects were not antagonized by flumazenil. The sedative effect was further confirmed in rats (10 mg/kg i.p.) and monkeys (1 mg/kg p.o.) by an increase of behavioral sleep and a corresponding electroencephalographic frequency spectral shift. Unlike the BZ hypnotics, U-90042 (10 mg/kg i.p.) produced no amnesia in the one-trial passive avoidance response in mice but antagonized diazepam-induced amnesia. In rats trained to discriminate an injection of diazepam from saline, U-90042 produced predominantly vehicle-appropriate responses, even at depressant doses. The in vivo diazepam-antagonist effect of U-90042 is consistent with its low intrinsic activity and diazepam-antagonism at the gamma-aminobutyric acidA alpha 1 beta 2 gamma 2 and alpha 3 beta 2 gamma 2 receptor subtypes. The receptor mechanism for the sedative/hypnotic effect is not clear at this time.
