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(-)-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
Molecular Weight:
337.37
MDL Number:
MFCD00082465
MOL File:
121917-57-5.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

(-)-MK-801 MALEATE Properties

storage temp. Store at -20°C
solubility DMSO: >20 mg/mL
form solid
color white
Water Solubility Soluble in water (25mM, gentle warming)
FDA UNII EF13O02IV0

SAFETY

Risk and Safety Statements

Safety Statements  22-24/25
WGK Germany  3
RTECS  HP1093575

(-)-MK-801 MALEATE price More Price(19)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 27213 (−)-MK-801 (maleate) 121917-57-5 10mg $61 2024-03-01 Buy
Cayman Chemical 27213 (−)-MK-801 (maleate) 121917-57-5 50mg $243 2024-03-01 Buy
Cayman Chemical 27213 (−)-MK-801 (maleate) 121917-57-5 5mg $32 2024-03-01 Buy
Cayman Chemical 27213 (−)-MK-801 (maleate) 121917-57-5 25mg $139 2024-03-01 Buy
Tocris 0955 (-)-MK801maleate ≥99%(HPLC) 121917-57-5 50 $399 2021-12-16 Buy
Product number Packaging Price Buy
27213 10mg $61 Buy
27213 50mg $243 Buy
27213 5mg $32 Buy
27213 25mg $139 Buy
0955 50 $399 Buy

(-)-MK-801 MALEATE Chemical Properties,Uses,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

Global( 124)Suppliers
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ATK CHEMICAL COMPANY LIMITED
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Henan Alfa Chemical Co., Ltd
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InvivoChem
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Nanjing Doge Biomedical Technology Co., Ltd
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View Lastest Price from (-)-MK-801 MALEATE manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
(-)-MK801MALEATE pictures 2020-02-02 (-)-MK801MALEATE
121917-57-5
US $1.00 / KG 1KG 99%HPLC 100KG Career Henan Chemical Co

(-)-MK-801 MALEATE Spectrum

(-)-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 less-active,transporters,()Dizocilpine maleate,Inhibitor,Dizocilpine,inhibit,NMDA,( ) Dizocilpine maleate,monoamine,Ionotropic glutamate receptors,iGluR,antidepressant (-)-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