| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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SDZ-220-581 (SDZ-220581; SDZ220581) is a novel and potent competitive antagonist of NMDA glutamate receptor subtype(pKi= 7.7) with the potential to be used for Parkinson's disease.
| 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].
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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. |
| References |
[1]. Urwyler S, Campbell E, Fricker G, 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 Jun;35(6):65
[2]. Gilmour G, et al. In vitro characterisation of the novel positive allosteric modulators of the mGlu₅ receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology. 2013 Jan;64:224-39. |
| Molecular Formula |
C16H17CLNO5P
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|---|---|
| Molecular Weight |
369.7378
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| Exact Mass |
369.0533
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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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| SMILES |
ClC1=CC=CC=C1C2=CC(C[C@@H](C(O)=O)N)=CC(CP(O)(O)=O)=C2
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| Synonyms |
SDZ220-581. SDZ-220581 SDZ 220-581 SDZ-220-581
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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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