Dizocilpine Maleate [(+)-MK 801 maleate]

Molecular Weight (MW)	337.37
Formula	C16H15N.C4H4O4
CAS No.	77086-22-7
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 68 mg/mL (201.6 mM)
Water: <1 mg/mL
Ethanol:<1 mg/mL
Other info	Chemical Name: 5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate InChi Key: QLTXKCWMEZIHBJ-BTJKTKAUSA-N InChi Code: InChI=1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1- SMILES Code: CC1(N2)C3=CC=CC=C3CC2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O
Synonyms	Dizocilpine; MK801; MK 801; MK-801; MK 801 Maleate

Molecular Weight (MW)

337.37

Formula

C16H15N.C4H4O4

CAS No.

77086-22-7

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 68 mg/mL (201.6 mM)

Water: <1 mg/mL

Ethanol:<1 mg/mL

Other info

Chemical Name: 5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate
InChi Key: QLTXKCWMEZIHBJ-BTJKTKAUSA-N
InChi Code: InChI=1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code: CC1(N2)C3=CC=CC=C3CC2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O

Synonyms

Dizocilpine; MK801; MK 801; MK-801; MK 801 Maleate

In Vitro	In vitro activity: (-)-Huperzine A is a novel alkaloid isolated from the Chinese herb Huperzia serrata. (-)-Huperzine A preferentially inhibits tetrameric AChE (G4 form). (-)-Huperzine A is more potent than tacrine, physostigmine, galanthamine, and rivastigmine with respect to inhibition of AChE activity, whereas HupA is the least potent BuChE inhibitor among the inhibitors. (-)-Huperzine A possesses the ability to protect cells against hydrogen peroxide, β-amyloid protein, glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis. These protective effects are related to its ability to attenuate oxidative stress, regulate the expression of apoptotic proteins Bcl-2, Bax, P53, and caspase-3, protect mitochondria, upregulate nerve growth factor and its receptors, and interfere with amyloid precursor protein metabolism. Cell Assay: izocilpine ((+)-MK 801) (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.
In Vivo	(-)-Huperzine A can ameliorate the learning and memory deficiency in animal models and AD patients. Its potentially beneficial actions include modification of β-amyloid peptide processing, reduction of oxidative stress, neuronal protection against apoptosis, and regulation of the expression and secretion of nerve growth factor (NGF) and NGF signaling. (-)-Huperzine A significantly inhibits AChE activity in the cortex, hippocampus, striatum, medial septum, medulla oblongata, cerebellum, and hypothalamus of rats that are killed 30 min following the administration of (-)-Huperzine A at several dose levels compared with the saline control.
Animal model	Male Sprague-Dawley rats
Formulation & Dosage	Dissolved in saline; 0.1mg/kg; oral gavage
References	Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8; Eur J Pharmacol. 1988 Jan 12;145(2):223-6; Brain Res. 2005 Jul 19;1050(1-2):190-8; Learn Mem.2008 Dec 2;15(12):857-65.

In Vitro

In vitro activity: (-)-Huperzine A is a novel alkaloid isolated from the Chinese herb Huperzia serrata. (-)-Huperzine A preferentially inhibits tetrameric AChE (G4 form). (-)-Huperzine A is more potent than tacrine, physostigmine, galanthamine, and rivastigmine with respect to inhibition of AChE activity, whereas HupA is the least potent BuChE inhibitor among the inhibitors. (-)-Huperzine A possesses the ability to protect cells against hydrogen peroxide, β-amyloid protein, glutamate, ischemia and staurosporine-induced cytotoxicity and apoptosis. These protective effects are related to its ability to attenuate oxidative stress, regulate the expression of apoptotic proteins Bcl-2, Bax, P53, and caspase-3, protect mitochondria, upregulate nerve growth factor and its receptors, and interfere with amyloid precursor protein metabolism.

Cell Assay: izocilpine ((+)-MK 801) (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.

In Vivo

(-)-Huperzine A can ameliorate the learning and memory deficiency in animal models and AD patients. Its potentially beneficial actions include modification of β-amyloid peptide processing, reduction of oxidative stress, neuronal protection against apoptosis, and regulation of the expression and secretion of nerve growth factor (NGF) and NGF signaling. (-)-Huperzine A significantly inhibits AChE activity in the cortex, hippocampus, striatum, medial septum, medulla oblongata, cerebellum, and hypothalamus of rats that are killed 30 min following the administration of (-)-Huperzine A at several dose levels compared with the saline control.

Animal model

Male Sprague-Dawley rats

Formulation & Dosage

Dissolved in saline; 0.1mg/kg; oral gavage

References

Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8; Eur J Pharmacol. 1988 Jan 12;145(2):223-6; Brain Res. 2005 Jul 19;1050(1-2):190-8; Learn Mem.2008 Dec 2;15(12):857-65.

CAS NO:	77086-22-7
规格:	≥98%

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
500mg	电议
1g	电议