| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
WAY-213613 targets the excitatory amino acid transporter 2 (EAAT2/GLT-1), a glutamate transporter highly expressed in both neurons and astrocytes. EAAT2 is responsible for the majority of glutamate uptake in the brain, maintaining low extracellular glutamate concentrations and preventing excitotoxicity. WAY-213613 inhibits EAAT2 with an IC₅₀ of 85 nM.
|
|---|---|
| ln Vitro |
The human EAAT1, EAAT2, and EAAT3 isoforms are inhibited by WAY-213613 (0-100 μM), with IC50 values of 5004 nM, 85 nM, and 3787 nM, respectively[1]. In the presence of 3, 30, and 300 nM, respectively, WAY-213613 (3, 30, 300 nM) inhibits synaptosomal L-[3H]glutamate absorption with Ki values of 15 nM, 41 nM, and 55 nM. [1]. In oocytes injected with EAAT1, EAAT2, or EAAT3, WAY-213613 (0-100 μM) generates concentration-dependent inhibition of glutamate-induced currents, with IC50 values of 48, 0.13, and 4.0 μM, respectively [1]. WAY-213613 (0.5–50 μM) exhibits strong action in inhibiting NMDA-stimulated responses and good selectivity for ionotropic receptors and EAAT2 [1].
In vitro, WAY-213613 is a potent and selective non-substrate reuptake inhibitor of EAAT2 with an IC₅₀ of 85 nM. It displays >44-fold selectivity over EAAT1 and EAAT3, with IC₅₀ values of 3787 nM and 5004 nM, respectively. The compound is used in methods for treating or inhibiting the onset of Huntington's disease with gene modulatory compounds. |
| ln Vivo |
In vivo activity data for WAY-213613 are limited in the available literature. As a research compound primarily used for in vitro studies, systematic in vivo efficacy studies have not been extensively reported. Its ability to inhibit glutamate uptake suggests potential for studying excitotoxicity and neurodegenerative conditions, but further in vivo studies are needed.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for WAY-213613 are not performed as traditional receptor binding assays, as it is a transporter inhibitor rather than a receptor ligand. Transport inhibition is assessed by measuring the uptake of radiolabeled glutamate or other substrates into cells or membrane preparations expressing EAAT2. The IC₅₀ (85 nM) is calculated from inhibition curves.
|
| Cell Assay |
In vitro cellular assays for WAY-213613 are performed using cells expressing EAAT2, such as primary astrocytes or neuronal cultures. Cells are treated with the compound, and glutamate uptake is measured using radiolabeled [³H]-glutamate or fluorescent glutamate analogues. The inhibition of glutamate uptake is quantified, and the IC₅₀ is calculated from concentration-response curves.
|
| Animal Protocol |
In vivo animal experimental protocols for WAY-213613 are not extensively documented. As a research compound, in vivo studies would typically involve administration to animal models of Huntington's disease or other neurodegenerative conditions. The compound would be administered via intraperitoneal or oral routes, and efficacy would be assessed by measuring glutamate levels, neuroprotection, and behavioral outcomes.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of WAY-213613 have been characterized in preclinical studies. The compound has a molecular weight of 415.19 and molecular formula C₁₆H₁₃BrF₂N₂O₄. It is soluble in DMSO at 83 mg/mL but insoluble in water and ethanol. For in vivo administration, it can be formulated as a homogeneous suspension in CMC-Na (≥5 mg/mL) or as a clear solution in 5% DMSO/40% PEG300/5% Tween 80/50% ddH₂O.
|
| Toxicity/Toxicokinetics |
Toxicological data for WAY-213613 are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
|
| References |
|
| Additional Infomation |
WAY-213613 is a research compound with a purity of 99.89%. It is also known as N4-[4-(2-Bromo-4,5-difluorophenoxy)phenyl]-L-asparagine. The compound is a selective GLT-1/EAAT2 inhibitor used in neuroscience research to study glutamate homeostasis, excitotoxicity, and neurodegenerative diseases. This product is for research use only.
|
| Molecular Formula |
C16H13BRF2N2O4
|
|---|---|
| Molecular Weight |
415.19
|
| Exact Mass |
414.003
|
| CAS # |
868359-05-1
|
| Related CAS # |
WAY-213613 hydrochloride;2450268-84-3
|
| PubChem CID |
11531745
|
| Appearance |
White to off-white solid powder
|
| Density |
1.665g/cm3
|
| Boiling Point |
565.634ºC at 760 mmHg
|
| Flash Point |
295.885ºC
|
| Index of Refraction |
1.632
|
| LogP |
4.033
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
25
|
| Complexity |
477
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1=CC(=CC=C1NC(=O)C[C@@H](C(=O)O)N)OC2=CC(=C(C=C2Br)F)F
|
| InChi Key |
BNYDDAAZMBUFRG-ZDUSSCGKSA-N
|
| InChi Code |
InChI=1S/C16H13BrF2N2O4/c17-10-5-11(18)12(19)6-14(10)25-9-3-1-8(2-4-9)21-15(22)7-13(20)16(23)24/h1-6,13H,7,20H2,(H,21,22)(H,23,24)/t13-/m0/s1
|
| Chemical Name |
(2S)-2-amino-4-[4-(2-bromo-4,5-difluorophenoxy)anilino]-4-oxobutanoic acid
|
| Synonyms |
WAY213613; WAY 213613; WAY-213613
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4085 mL | 12.0427 mL | 24.0854 mL | |
| 5 mM | 0.4817 mL | 2.4085 mL | 4.8171 mL | |
| 10 mM | 0.2409 mL | 1.2043 mL | 2.4085 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.