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BioChemicals
Neu2000
tcsc0025740
Neu2000
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AVAILABLE SIZES
1mg
5mg
10mg
50mg
100mg
$
189.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product 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 IC
50
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 EC
50
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 C
max
(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]
.
Information
CAS No
640290-67-1
Formula
C
15
H
8
F
7
NO
3
Clinical Information
clinicalinformation
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Target
iGluR
iGluR
Specifications
Purity / Grade
>98%
Solubility
DMSO : ≥ 112.5 mg/mL (293.57 mM)
Smiles
smiles
Misc Information
Observed Molecular Weight
383.22
related data
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