| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
SDZ-220-581 targets the NMDA glutamate receptor, acting as a potent and competitive antagonist. It exhibits a pKi of 7.7 for the NMDA receptor. The compound is also described as a platelet-activating factor (PAF) receptor antagonist. By blocking NMDA receptors, SDZ-220-581 modulates glutamatergic neurotransmission, which is implicated in various neurological and psychiatric disorders.
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| ln Vitro |
In vitro, SDZ-220-581 acts as a potent and competitive NMDA receptor antagonist with a pKi of 7.7. Its activity is typically assessed in receptor binding assays measuring affinity for the NMDA receptor and in functional assays measuring inhibition of NMDA-induced currents or calcium influx. The compound's selectivity for NMDA over other glutamate receptor subtypes can also be evaluated.
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| ln Vivo |
Male OF-1 mice were dose-dependently protected against maximal electroshock epileptic seizures (MES) by treatment with SDZ 220-581 (3.2–32 mg/kg; p.o.; for 24 hours). The quick onset and extended duration of action of SDZ 220-581 are characteristics of its protective duration [1].
In vivo, SDZ-220-581 reversed haloperidol-induced catalepsy in rats, a widely used model of Parkinson's disease. This demonstrates its ability to modulate NMDA receptor-mediated neurotransmission in the central nervous system. The compound's oral activity supports its utility for studying NMDA receptor function in neurological disorders. |
| Enzyme Assay |
In cell-free receptor binding assays, SDZ-220-581's activity is evaluated by measuring its affinity for the NMDA receptor. Membrane preparations from brain tissue or cells expressing NMDA receptors are incubated with radiolabeled ligands (e.g., [3H]MK-801 or [3H]CGP-39653) and varying concentrations of SDZ-220-581. The displacement of the radioligand is measured, and the pKi (7.7) is calculated from the competition curve.
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| Cell Assay |
In vitro cell-based experiments with SDZ-220-581 typically involve primary neuronal cultures or cell lines expressing NMDA receptors. Cells are treated with the compound in the presence of NMDA, and receptor activation is assessed by measuring intracellular calcium influx using fluorescent dyes or by electrophysiological techniques. The inhibition of NMDA-induced responses is measured to determine the compound's antagonist potency.
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| Animal Protocol |
Animal/Disease Models: Male OF-1 mouse (18-26g) [1]
Doses: 3.2mg/kg, 10mg/kg, 32mg/kg Route of Administration: Oral administration; Route of Administration: Oral administration. 24-hour Experimental Results: Dose-dependent protection of mice from maximal electroshockable seizures (MES) following oral administration. In vivo animal experiments with SDZ-220-581 have been conducted in rat models of Parkinson's disease. In typical protocols, rats are treated with haloperidol to induce catalepsy, and then SDZ-220-581 is administered. The reversal of catalepsy is measured using the bar test or other behavioral assays. The compound's effects on motor function and NMDA receptor-mediated behaviors are assessed. |
| ADME/Pharmacokinetics |
SDZ-220-581 is an orally active compound. Its pharmacokinetic properties include oral bioavailability and distribution to the central nervous system. The compound has a molecular formula of C16H17ClNO5P and a molecular weight of 369.74. Its half-life and metabolic profile have not been extensively characterized.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for SDZ-220-581. In preclinical studies, the compound has shown efficacy in reversing haloperidol-induced catalepsy without reported significant toxicity. The compound is for research use only and is not intended for human therapeutic applications.
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| References |
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| Additional Infomation |
SDZ-220-581 has a molecular formula of C16H17ClNO5P and a molecular weight of 369.74. Its chemical name is (alphaS)-alpha-Amino-2'-chloro-5-(phosphonomethyl)(1,1'-biphenyl)-3-propanoic acid. It is a potent, orally active, and competitive NMDA receptor antagonist with a pKi of 7.7. The compound reversed haloperidol-induced catalepsy in rats and is also described as a PAF receptor antagonist. It is available for research purposes only.
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| Molecular Formula |
C16H17CLNO5P
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| Molecular Weight |
369.7378
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| Exact Mass |
369.053
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| CAS # |
174575-17-8
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| Related CAS # |
SDZ 220-581 Ammonium salt;179411-94-0;SDZ 220-581 hydrochloride;179411-93-9
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| PubChem CID |
128019
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
613.3±65.0 °C at 760 mmHg
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| Flash Point |
324.7±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
0.89
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
485
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C(C(=C1)C2=CC(=CC(=C2)CP(=O)(O)O)C[C@@H](C(=O)O)N)Cl
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| InChi Key |
VBRJFXSFCYEZMQ-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C16H17ClNO5P/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)/t15-/m0/s1
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| Chemical Name |
(2S)-2-amino-3-[3-(2-chlorophenyl)-5-(phosphonomethyl)phenyl]propanoic acid
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| Synonyms |
SDZ220-581. SDZ-220581 SDZ 220-581 SDZ-220-581
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~8.57 mg/mL (~23.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7046 mL | 13.5230 mL | 27.0460 mL | |
| 5 mM | 0.5409 mL | 2.7046 mL | 5.4092 mL | |
| 10 mM | 0.2705 mL | 1.3523 mL | 2.7046 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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