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Merck

5.05764

NMDA Antagonist XI, N1-dansyl-spermine

別名:

NMDA Antagonist XI, N1-dansyl-spermine, NMDA channel blocker, N1-dansyl-spermine, N1-DnsSpm

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この商品について

実験式(ヒル表記法):
C22H37N5O2S · 3HCl
分子量:
545.01
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
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assay

≥97% (HPLC)

Quality Segment

form

powder

potency

0.31 μM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow-white

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

SMILES string

CN(C)C1=CC=CC2=C1C=CC=C2S(=O)(=O)NCCCNCCCCNCCCN

InChI

1S/C22H37N5O2S/c1-27(2)21-11-5-10-20-19(21)9-6-12-22(20)30(28,29)26-18-8-17-25-15-4-3-14-24-16-7-13-23/h5-6,9-12,24-26H,3-4,7-8,13-18,23H2,1-2H3

InChI key

NSUSGNAFCIMCDH-UHFFFAOYSA-N

General description

An N-sulfonyl-polyamine that acts as a potent and more specific antagonist of NMDA receptors expressed in Xenopus oocytes (IC50 = 310, 340 nM in NR1/NR2A and NR1/NR2B, respectively). The inhibition appears to be voltage-dependent and is non-competitive with respect to glutamate and glycine. Exhibits about 50-fold greater selectivity over NR1/NR2C and NR1/NR2D receptors (IC50 = 16 and 13 µM, respectively). Also shown to block c-AMP-dependent, calmodulin-activated phosphodiesterase (IC50 = 58 µM) and diminishes the induction of ornithine decarboxylase. At higher concentration (˜100 µM) it is shown to reduce spontaneous epileptiform activity in mouse cortical slices.

Biochem/physiol Actions

Primary Target
NMDA

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Kirby, B.P., et al. 2005, Eur. J. Pharmacol. 524, 53.
Li, J., et al. 2005, Brain Res. 1055, 180.
Kirby, B. et al. 2004, Brain Res. 1011, 69.
Seiler, N., et al. 1998, J. Biochem. Cell Biol. 30, 393.

Chao, J., et al. 1997, Mol. Pharm. 51, 861.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)


保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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