SDZ 220-581 hydrochlorideNMDA receptor antagonist CAS# 179411-93-9 |
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Quality Control & MSDS
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| Cas No. | 179411-93-9 | SDF | Download SDF |
| PubChem ID | 78357772 | Appearance | Powder |
| Formula | C16H18Cl2NO5P | M.Wt | 406.2 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 5 mg/mL (12.31 mM; Need ultrasonic and warming) | ||
| Chemical Name | (2S)-2-amino-3-[3-(2-chlorophenyl)-5-(phosphonomethyl)phenyl]propanoic acid;hydrochloride | ||
| SMILES | C1=CC=C(C(=C1)C2=CC(=CC(=C2)CP(=O)(O)O)CC(C(=O)O)N)Cl.Cl | ||
| Standard InChIKey | WSYIMHDAUSNYSF-RSAXXLAASA-N | ||
| Standard InChI | InChI=1S/C16H17ClNO5P.ClH/c17-14-4-2-1-3-13(14)12-6-10(8-15(18)16(19)20)5-11(7-12)9-24(21,22)23;/h1-7,15H,8-9,18H2,(H,19,20)(H2,21,22,23);1H/t15-;/m0./s1 | ||
| 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 | SDZ 220-581 Hcl is a potent, competitive antagonist at the NMDA glutamate receptor subtype(pKi= 7.7).
IC50 Value:
Target: NMDA receptor
in vitro: Wake-promoting doses of LSN2463359 and LSN2814617 attenuated deficits in performance induced by the competitiveNMDA receptor antagonist SDZ 220,581 in two tests of operant behaviour: the variable interval 30 s task and the DMTP task [1].
in vivo: Administration of SDZ 220-581 or CGS 19755 was associated with a robust reduction in PPI, whereas L-701,324, 4-Cl-KYN or MLA failed to alter PPI [2]. With the most active agent, SDZ 220-581, full protection against maximal electroshock seizures (MES) was obtained at oral doses of 10 mg/kg in rats and in mice. The compound had a fast onset (< or = 1 hr) and a long duration (> or = 24 hr) of action [3]. Rats were pretreated with clozapine (0 or 5.0 mg/kg) or haloperidol (0 or 0.1 mg/kg), together with SDZ 220-581 (0 or 2.5 mg/kg), and tested. SDZ 220-581 and SDZ EAB-515 decreased PPI without affecting startle magnitude [4]. References: | |||||
SDZ 220-581 hydrochloride Dilution Calculator
SDZ 220-581 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4618 mL | 12.3092 mL | 24.6184 mL | 49.2368 mL | 61.546 mL |
| 5 mM | 0.4924 mL | 2.4618 mL | 4.9237 mL | 9.8474 mL | 12.3092 mL |
| 10 mM | 0.2462 mL | 1.2309 mL | 2.4618 mL | 4.9237 mL | 6.1546 mL |
| 50 mM | 0.0492 mL | 0.2462 mL | 0.4924 mL | 0.9847 mL | 1.2309 mL |
| 100 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.4924 mL | 0.6155 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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SDZ 220-581 hydrochloride is a potent and competitive antagonist of NMDA receptor with pKi value of 7.7 [1].
SDZ 220-581 is a biphenyl-AP7-derivative. It is potent both in vitro and in vivo. SDZ 220-581 binds with high affinity to the recognition site of NMDA receptor. It does not bind to the strychnine-insensitive glycine site or the MK-801 site within the NMDA receptor. In addition, SDZ 220-581 shows no effect on a variety of other binding assays such as for dopamine, serotonin and adenosine [1].
In the in vivo assay, the administration of SDZ 220-581 protects the mice against the maximal electroshock-induced seizures (MES). In the rat MES model, SDZ 220-581 also shows potent efficacy. Moreover, SDZ 220-581 can protect brain against quinolinic acid induced neuronal degeneration in rat. Furthermore, a dose of 1.25mg/kg SDZ 220-581 markedly reduces the cerebral infarct size in the focal cerebral ischemia model in rat [2].
References:
[1] Urwyler et al .Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitive N-methyl-D-aspartate receptor antagonists - II. Pharmacological characterization in vivo. Neuropharmacology 1996, 35 655.
[2] Urwyler S, Campbell E, Fricker G, et al. Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitiveN-Methyl-D-aspartate receptor antagonists—II. Pharmacological characterization in vivo[J]. Neuropharmacology, 1996, 35(6): 655-669.
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