| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
EAAT2
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|---|---|
| ln Vitro |
With IC50 values of 5004 nM, 85 nM, and 3787 nM, respectively, WAY-213613 hydrochloride (0-100 μM) exhibits inhibitory activity against human EAAT1, EAAT2, and EAAT3 isoforms[1]. With Ki values of 15 nM, 41 nM, and 55 nM, WAY-213613 hydrochloride (3,30,300 nM) inhibits synaptosome L-[3H] glutamate absorption [1]. When EAAT1-, EAAT2-, or EAAT3 is injected into oocytes, WAY-213613 hydrochloride (0-100 μM) blocks glutamate-induced currents in a concentration-dependent manner (IC50 values: 48, 0.13, and 4.0 μM, respectively)[1]. With strong selectivity for ionophilic receptors and EAAT2, WAY-213613 hydrochloride (0.5-50 μM) exerts inhibiting effects on NMDA stimulation responses [1].
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| References |
[1]. Dunlop J, et al. Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2. Mol Pharmacol. 2005 Oct;68(4):974-82. Epub 2005 Jul 13.
[2]. Simmons DA, et al. A small molecule p75NTR ligand, LM11A-31, reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression. PLoS One. 2014 Aug 25;9(8):e102136. |
| Molecular Formula |
C16H14BRCLF2N2O4
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|---|---|
| Molecular Weight |
451.65
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| CAS # |
2450268-84-3
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| Related CAS # |
WAY-213613;868359-05-1
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| SMILES |
C1(=CC(Br)=C(C=C1F)OC1C=CC(NC(=O)C[C@@H](C(=O)O)N)=CC=1)F.Cl
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (110.71 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.54 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 (5.54 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 (5.54 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 | 2.2141 mL | 11.0705 mL | 22.1410 mL | |
| 5 mM | 0.4428 mL | 2.2141 mL | 4.4282 mL | |
| 10 mM | 0.2214 mL | 1.1071 mL | 2.2141 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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