1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. Neu2000

Neu2000 

Cat. No.: HY-106408 Purity: 99.09%
Handling Instructions

Neu2000 is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist.

For research use only. We do not sell to patients.

Neu2000 Chemical Structure

Neu2000 Chemical Structure

CAS No. : 640290-67-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 334 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

Neu2000 is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist.

IC50 & Target

NMDA receptor[1]

In Vitro

Neu2000 shows apparent neuroprotection against 300 μM N-methyl-D-aspartate (NMDA) at doses as low as 30 μM. Neu2000 does not protect cortical neurons against α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid- or kainate-mediates excitotoxicity. Neu2000 inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner, indicating that the effect is mediated by a specific action at NMDA receptors. The Neu2000 dose-response has an IC50 of 35.38±5.94 μM and Hill's coefficient of 0.91 (n=8). Neu2000 (100 μM) significantly reduces the maximal NMDA response by 58.31±2.72% (n=5) and the EC50 values of NMDA from 18.88±1.85 to 9.92±0.17 μM (n=5, P<0.05)[1].

In Vivo

Pharmacokinetic analysis reveals that the half-life of Neu2000 is 1.42, 2.14, and 1.79 h following intraperitoneal administration of 10, 25, and 50 mg/kg, respectively. In addition, the Cmax (maximum plasma concentration) is calculated as 3.86, 18.73, and 52.83 μg/mL and the AUC (area under the curve) is determined to be 7.37, 55.15, and 96.77 μg/h/mL at the same respective doses. The levels of basal mitochondrial ROS are significantly elevated at 24 h post-surgery in both the vehicle-treated (4.1-fold, p<0.01) and Neu2000-treated (2.9-fold, p<0.01) groups compare to sham controls. The results of blood-brain barrier (BBB) test also reveals significant changes in open field locomotion in spinal cord-injured animals treated with Neu2000 compare to vehicle-treated animals. Single (p<0.05) or repeated (p<0.01) Neu2000 treatment results in a decreased swing to stance ratio compare to vehicle-treated animals. Repeated treatment with Neu2000 results in a 45.6% decrease (p<0.01) in overall lesion volume compare to vehicle treatment, while a single administration of Neu2000 results in a 36.8% decrease (p<0.05) in overall lesion volume[2].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 112.5 mg/mL (293.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6095 mL 13.0473 mL 26.0947 mL
5 mM 0.5219 mL 2.6095 mL 5.2189 mL
10 mM 0.2609 mL 1.3047 mL 2.6095 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Whole-cell voltage-clamp recordings are performed on primary cultured cortical neurons (11 to 14 DIV) at room temperature (18°C to 23°C). Whole-cell currents are recorded and analyzed using an amplifier. The 2 to 3-MΩ-resistance recording pipettes are filled with an internal solution containing 135 mM CsCl, 10 mM N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid, 1.2 mM MgCl2, 4 mM ATP-Na2, 0.5 mM CaCl2, and 11 mM ethyleneglycol tetraacetate (pH adjusted to 7.3 with CsOH). The external solution is composed of 140 mM NaCl, 2 mM KCl, 2 mM CaCl2, 10 mM N-2-hydroxyethylpiperazine-N′-2-ethanesulfonic acid, and 0.01 mM glycine (pH adjusted to 7.3 to 7.4 with NaOH). N-methyl-D-aspartate and Neu2000 solutions are prepared by dissolving these chemicals in the external solutions, and they are applied to target neurons using a gravity-driven superfusion system with a linear array of 8 to 10 barrels. Graphing of data and dose-response analysis are performed and all data are presented as mean±s.e[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

The pharmacokinetic profile of Neu2000 in normal rats is examined using intraperitoneal (ip) route of administration. Rats are anesthetized by ether inhalation and the femoral artery cannulated. Rats are placed into cages for 1 h and then receive injections (10, 25, or 50 mg/kg ip, n=6 per dose) of Neu2000 dissolved in sterile saline. Blood is collected from the femoral artery at 15, 30, 60, 120, 240, 480, and 1440 min following injection. Plasma aliquots of 50 μL are spiked with 100 μL of internal standard solution (Neu2000IS, 10 μg/mL in acetonitrile). After vortex mixing for 1 min, the samples are centrifuged at 12,000 g for 5 min. A total of 50 μL of the supernatant phase is separated and diluted with 50 μL of distilled water. Plasma concentrations relative to time are obtained using liquid chromatography-mass spectrometry[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

383.22

Formula

C₁₅H₈F₇NO₃

CAS No.

640290-67-1

SMILES

OC(C1=C(O)C=CC(NCC2=C(C(F)=C(C(F)(F)F)C(F)=C2F)F)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.09%

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Cat. No.:
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Cat. No.: HY-106408