ChemicalBook > CAS DataBase List > (-)-MK-801 MALEATE

(-)-MK-801 MALEATE

Product Name
(-)-MK-801 MALEATE
CAS No.
121917-57-5
Chemical Name
(-)-MK-801 MALEATE
Synonyms
CS-2146;(-)-MK 801;(-)-Dizocilpine;(-)-MK801MALEATE;(-)MK-801 maleate;(-)-MK-801 MALEATE;MK 801;MK801;C13737;(-)-DIZOCILPINE MALEATE;(-)-MK-801 MALEATE USP/EP/BP;(-)-Dizocilpine Maleate [(-)-MK 801 maleate
CBNumber
CB5407484
Molecular Formula
C20H19NO4
Formula Weight
337.37
MOL File
121917-57-5.mol
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(-)-MK-801 MALEATE Property

storage temp. 
Store at -20°C
solubility 
DMSO: >20 mg/mL
form 
solid
color 
white
Water Solubility 
Soluble in water (25mM, gentle warming)
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Safety

Safety Statements 
22-24/25
WGK Germany 
3
RTECS 
HP1093575
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
27213
Product name
(−)-MK-801 (maleate)
Packaging
10mg
Price
$61
Updated
2024/03/01
Cayman Chemical
Product number
27213
Product name
(−)-MK-801 (maleate)
Packaging
50mg
Price
$243
Updated
2024/03/01
Cayman Chemical
Product number
27213
Product name
(−)-MK-801 (maleate)
Packaging
5mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
27213
Product name
(−)-MK-801 (maleate)
Packaging
25mg
Price
$139
Updated
2024/03/01
Tocris
Product number
0955
Product name
(-)-MK801maleate
Purity
≥99%(HPLC)
Packaging
50
Price
$399
Updated
2021/12/16
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(-)-MK-801 MALEATE Chemical Properties,Usage,Production

Uses

(-)-MK 801 Maleate was used in biological study to observe antipsychotics and other agents effects on prepulse inhibition of acoustic startle in rats. Binding properties of (-)-MK 801 Maleate, NMDA receptor channel blocker, were characterized in different brain regions

Biological Activity

(+)-mk 801 maleate is a potent antagonist of nmda with ki value of 30.5nm [1].mk 801 is a potent anticonvulsant exhibits both anxiolytic and sympathomimetic properties. it is found to be a noncompetitive antagonist of nmda. mk 801 can penetrate into the central nervous system. in the in vitro assay, mk 801 binds to rat cerebral cortical membrane with high affinity in a saturable manner. this binding is reversible even when the concentration of mk 801 is up to 100μm. it is also found that the binding shows a regional specificity. most of these binding sites are located in the hippocampus. in rat cortical-slice preparations, mk 801 causes a potent blockade of depolarizing responses to nmda with a high selectivity. this effect is persistent. the blockade can also cause a suppression of the epileptiform activity induced by tetrodotoxin or other neurotoxin [1].

in vitro

[3H]MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. It produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for [3H]MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype. MK-801 inhibits N-methyl-D -aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively. MK- 801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK -801 is applied for a long time in the presence of NMDA. MK-801 is also effective at blocking NMDA-activated single-channel activity in outside-out patches. MK-801 (< 500 μM) prevents LPS-induced activation of microglia in a conce ntration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells.

in vivo

Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduced the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice. MK-801 (0.05 mg/kg or 0.2 mg/kg, ip) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurs in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, ip) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement.

target

TargetValue
NMDA receptor 30.5 nM(Ki)

storage

Room temperature

References

[1] wong eh, kemp ja, priestley t, knight ar, woodruff gn, iversen ll . the anticonvulsant mk-801 is a potent n-methyl-d-aspartate antagonist. proc natl acad sci u s a. 1986 sep;83(18):7104-8.

(-)-MK-801 MALEATE Preparation Products And Raw materials

Raw materials

Preparation Products

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(-)-MK-801 MALEATE Suppliers

China 104 Germany 1 India 1 Italy 1 Japan 1 Switzerland 1 United Kingdom 4 United States 11 Global 124
Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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sales@boylechem.com
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China
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3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
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86-21-50328109
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3bsc@sina.com
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China
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ZHIWE CHEMTECH CO LTD
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021-20221225 13917446399
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QQ:115820162
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sales@zhiwe.net
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China
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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meilunui@163.com
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China
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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info@chemexpress.com
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Shanghai Aladdin Bio-Chem Technology Co.,LTD
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400-400-6206333 18521732826
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market@aladdin-e.com
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MedChemexpress LLC
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021-58955995
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609-228-5909
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sales@medchemexpress.cn
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United States
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Clearsynth Labs Limited
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+91-22-26355700
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+91-22-26355701
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info@clearsynth.com
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India
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TargetMol Chemicals Inc.
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021-021-33632979 15002134094
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021-33632979
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marketing@targetmol.com
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China
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AdooQ Bioscience CHINA
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025-58849295 18951903616;
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025-68650336
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info@adooq.cn
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China
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2990
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View Lastest Price from (-)-MK-801 MALEATE manufacturers

Career Henan Chemical Co
Product
(-)-MK801MALEATE 121917-57-5
Price
US $1.00/KG
Min. Order
1KG
Purity
99%HPLC
Supply Ability
100KG
Release date
2020-02-01

121917-57-5, (-)-MK-801 MALEATERelated Search:

Argatroban (-)-MK 801 MALEATE, >99% (-)-MK 801 MALEATE,(+)-MK 801 MALEATE (-)-MK-801 MALEATE (S)-(-)-N-Benzyl-1-phenylethylamine 1,1-DIMETHYL-1,2,3,4-TETRAHYDROISOQUINOLINE 10,11-DIHYDRO-5 H-DIBENZO[A,D]CYCLOHEPTENE 1-Phenyl-1,2,3,4-tetrahydro-isoquinoline 10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine ALPHA,ALPHA'-DIMETHYLDIBENZYLAMINE 3-METHYL-1,2,3,4-TETRAHYDROISOQUINOLINE (R)-(+)-N-Benzyl-1-phenylethylamine (2-methylphenyl)(phenyl)methylamine (-)-MK-801 MALEATE

  • (-)-MK-801 MALEATE
  • (-)-MK 801
  • (5R)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine (Z)-2-butenedioate
  • (5S,10R)-(-)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE MALEATE
  • (-)-MK801MALEATE
  • 5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5R,10S)-, (2Z)-2-butenedioate (1:1)
  • MK 801;MK801;C13737
  • 5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5R,10S)
  • (-)-DIZOCILPINE MALEATE
  • CS-2146
  • (-)MK-801 maleate
  • (-)-MK-801 MALEATE USP/EP/BP
  • (-)-Dizocilpine Maleate [(-)-MK 801 maleate
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  • (-)-Dizocilpine
  • (5R,10S)-5-Methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate
  • 121917-57-5
  • Cell Biology
  • Cell Signaling and Neuroscience
  • BioChemical
  • Ion Channels
  • Ionotropic Glutamate Receptor Modulators
  • Ligand-Gated Ion Channels
  • Inhibitors