Download Neuroscience-Alzheimer`s products (, 1.78 kB)

MAR2011
Neuroscience Products:
Inhibitors, Substrates, Agonists, and Antagonists
Cayman offers a select group of research tools (inhibitors and substrates as well as receptor agonists and
antagonists) pertinent to Neuroscience research areas such as Alzheimer’s disease and pain management as well
as more general factors related to excitatory and inhibitory signal transduction.
Item No.
78050
Product Name
(-)-(α)-Kainic Acid
Notes
Developed as the prototype neuroexcitatory amino acid for the induction of seizures in
experimental animals
13644
Aspalatone
Generates antioxidant and neuroprotective effects against kainic acid-induced epilepsy in
rat hippocampus
10008346
Gabapentin
A GABA analog
13623
Topiramate
A sugar sulfamate that exhibits potent anticonvulsant activity
13667
Muscimol
A full GABAA agonist and partial GABAC agonist
10032
N-(α-Linolenoyl) Tyrosine
A simple a-amide conjugate prepared as a method for CNS dopamine content by
facilitated transport of the tyrosine precursor across the blood-brain barrier
13248
L-DOPA
A metabolic precursor of dopamine that is capable of crossing the blood-brain barrier
13205
Halopemide
A potent inhibitor of phospholipase D and dopamine receptors
10488
Bupropion (hydrochloride)
An inhibitor of dopamine and norepinephrine reuptake and an antagonist of neuronal
13358
CAY10608
A potent, selective, and non-competitive antagonist of the NR2B subunit of NMDA receptors
10010743
Capsaicin (technical grade)
The primary active component of the heat and pain-eliciting lipid-soluble fraction of the
acetylcholine nicotinic receptors
Capsicum pepper
92350
Capsaicin
The primary active component of the heat and pain-eliciting lipid-soluble fraction of the
Capsicum pepper
92355
Dihydrocapsaicin
A major impurity found in natural hot pepper extracts
90052
Arvanil
A structural analog of capsaicin
90262
Olvanil
A structural analog of capsaicin
10005633
CAY10448
A potent capsaicin receptor antagonist
10007518
Capsazepine
A competitive antagonist of TRPV1
To view Cayman’s entire line
10009501
20-hydroxy
A potential CYP450 metabolite of N-arachidonoyl taurine that may activate
of Neuroscience products,
N-Arachidonoyl Taurine
members of the TRP family of calcium channels
10012565
CAY10568
A physically smaller, less hydrophobic version of QX314 designed to be more permeable
10137
Icilin
70090
BW 723C86
A 5-HT receptor agonist with 10-fold selectivity for the HT2B receptor
13203
Agomelatine
A metabolically stable analog of melatonin a competitive antagonist of 5-HT2C and
request a copy of the
to TRPV1 ion channel
Neuroscience catalog
A synthetic CMR1/TRPM8 super agonist that serves as a reference cold nociceptive
agonist for TRP-type ion channels
5-HT2B receptors
10011546
AL 34662
A potent 5-HT2 receptor agonist with ocular hypotensive activity
10096
SB 242084 (hydrochloride)
An antagonist of the 5-HT2C receptor
10005254
AFMK
A melatonin metabolite that has antioxidant and free radical scavenging activities
90377
13-Docosenamide
The amide of docosenoic acid identified in the CSF of sleep-deprived cats
10012588
A-803467
A sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8
10009312
SKF-96365 (hydrochloride)
Inhibits the receptor-mediated influx of calcium via voltage-gated calcium channels
10010109
8-DY547-cGMP
A fluorescently-labeled cyclic nucleotide used to study CNGA2 channel activation
10011135
BAY-60-7550
A potent type 2 cyclic nucleotide phosphodiesterases (PDE2) inhibitor
10011126
Clobenpropit (hydrobromide)
A selective histamine H3 receptor antagonist that crosses the blood-brain barrier
10011127
Thioperamide Maleate
A selective histamine H3 receptor antagonist that crosses the blood-brain barrier
9000849
Phenazepam
A benzodiazepine agonist of the GABAA-benzodiazepine receptor chloride channel complex
sodium channels
For full information on these products and more, visit caymanchem.com
Alzheimer’s Disease
Methyltransferase Activity
Insoluble deposits of β-amyloid peptide (Aβ) and hyperphosphorylation
of the microtubule-associated tau protein leads to the aggregation and
formation of amyloid plaques and neurofibrillary tangles, both hallmarks
of Alzheimer’s disease. In an effort to support the necessary research to
prevent and treat the symptoms of this degenerative disease, Cayman
offers a collection of tools that target the inhibition of β-amyloid peptide
production and aggregation, as well as the prevention of tau protein
phosphorylation and modification. Additional compounds purport to stave
off dementia and improve cognitive function by targeting other various
signaling pathways.
Methylation of key biological molecules and proteins play important roles in numerous
biological systems. S-adenosylmethionine (SAM) dependent methyltransferases use SAM,
also known as AdoMet, to donate a methyl group that is required for the modification of
proteins and DNA. Aberrant levels of SAM have been linked to many abnormalities, including
Alzheimer’s disease, depression, Parkinson’s disease, multiple sclerosis, liver failure, and cancer.
Methyltransferase Fluorometric Assay Kit
700150
The β-amyloid peptide is derived from sequential proteolytic cleavage of the amyloid precursor
protein (APP) by β- and γ-secretases. Initial cleavage by β-secretase (BACE), a membrane
anchored aspartic protease, generates a soluble N-terminal fragment and a membrane-associated
C-terminal fragment. The C-terminal fragment then undergoes proteolysis by γ-secretase to
give the Aβ peptide.
Cayman’s Methyltransferase Fluorometric Assay Kit
is an enzyme-coupled assay that can continuously
monitor SAM-dependent methyltransferases. The
removal of the methyl group from SAM generates
S-adenosylhomocysteine (AdoHcy), which is rapidly
converted to S-ribosylhomocysteine and adenine
by AdoHcy nucleosidase. This rapid conversion
prevents the buildup of AdoHcy and its feedback
inhibition on the methylation reaction. Finally, the adenine is converted to hypoxanthine,
by adenine deaminase, which in turn is converted to urate and hydrogen peroxide (H2O2).
The reaction between H2O2 and ADHP (10-acetyl-3,7,-dihydroxyphenoxazine) produces
the highly fluorescent compound resorufin. Resorufin fluorescence can be easily analyzed
with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.
β-Amyloid (1-8, A2V) Peptide
Methyltransferase Colorometric Assay Kit
14,000
Fluorescence (Relative Units)
12,000
10,000
8,000
6,000
4,000
2,000
0
0
b-Amyloid
10
20
40
30
Time (min)
Cayman’s Methyltransferase Colorimetric Assay
Kit operates on a similar principle as the above
fluorometric kit except the rate of production of
H2O2 is measured with the colorimetric reagent,
3,5-dichloro-2-hydroxybenzenesulfonic acid, by an
increase in absorbance at 500-520 nm.
700140
0.450
0.400
0.350
Absorbance (515 nm)
10229
Aβ, Aβ 1-8 mutant, β-amyloid (1-8) dominant negative
β-Amyloid peptide (1-42) aggregation results in the formation of neurotoxic fibrils or globular
oligomers. The amyloid precursor protein (APP) mutation Ala673 → Val673 results in disease for
homozygous carriers but not for heterozygous carriers. The mutation generates β-amyloid peptide
with valine at amino acid position two. Biochemical analysis of Aβ (1-42) aggregation suggests
this small peptide may be a useful guide for developing β-amyloid peptide aggregation inhibitors.
0.300
0.250
0.200
0.150
0.100
0.050
0.000
0
• Also Available: b-Amyloid (1-8) Peptide (10241)
5
10
15
20
25
30
35
Time (min)
BACE (human recombinant)
10227
ASP-2, BACE-1, Memapsin, Membrane-bound Aspartic Protease, b-Secretase
Purity: ≥95% Summary: Source: human recombinant C-terminal His-tag protein purified
from E. coli • Mr: 48 kDa
BACE Inhibitor Screening Assay Kit
600070
BACE, the major β-secretase, initiates the
first step in β-amyloid peptide production.
Inhibition of BACE activity could potentially
block the entire cascade of Alzheimer’s disease
pathogenesis. Cayman’s BACE Inhibitor
Screening Assay Kit provides a convenient
method for screening human BACE inhibitors.
The assay utilizes a synthetic Swedish mutant APP
peptide (EVNLDAEF) that has been linked to a
fluorophore (EDANS) at one end and to a quenching agent (Dabcyl) at the other. After
cleavage by BACE, the product (peptide-EDANS) is brightly fluorescent and can be easily
analyzed using a fluorescence plate reader or a fluorometer with excitation wavelengths of
335-345 nm and emission wavelengths of 485-510 nm.
120
100
% Initial Activity
80
60
40
20
0
-20
0
100
10
Inhibitor (nM)
1,000
Methionine Sulfoxide
Protein methionine sulfoxide (MetO) is a reversible oxidative modification that occurs by
exposure of protein(s) methionine residues to reactive oxygen species (ROS). Methionine
oxidation can alter the function(s) of the modified proteins and if not reversed by MetO
reductases can be further oxidized to methionine sulfone, an irreversible modification. The
overabundance of methionine sulfoxidation is implicated in age-related diseases.
Methionine Sulfoxide Immunoblotting Kit
600160
Cayman’s MetO Immunoblotting Kit contains reagents needed for the immunochemical
detection of proteins containing MetO residues by western blotting. MetO-containing
samples of interest include those from cell or tissue lysates as well as semi-pure or purified
proteins. Samples may be prepared with reducing or non-reducing sample buffer prior
to SDS-PAGE and tested alongside one SDS-PAGE well designated for the provided
positive control. The MetO Polyclonal Antibody was isolated from rabbit serum generated
after immunization with a oxidized corn protein (MetO-DZS18) rich in methionine.
This polyclonal antibody is specific for protein methionine sulfoxide and can detect IgGcontaining MetO from sera of Alzheimer’s patients but not from normal control sera.
Additional Compounds
Item No.
Product Name
Notes
13332
(S)-Glycyl-H-1152 (hydrochloride)
A selective, potent Rho kinase IV inhibitor derived from HA-1077 (Fasudil)
70240
Tacrine (hydrochloride)
A derivative of aminoacridine which functions as an inhibitor of both AChE and butyrylcholinesterase
10005836
bis(7)-Tacrine
An AChE inhibitor that is 1,000 times more potent than tacrine
13245
Donepezil
A reversible AChE inhibitor that readily crosses the blood-brain barrier to reduce the breakdown of acetylcholine
13662
Arecoline (hydrobromide)
An agonist of the muscarinic acetylcholine receptors M1, M2, and M3
10230
(+)-Muscarine (iodide salt)
The biologically active stereoisomer of muscarine
9000556
Dimebolin
A non-selective antihistamine that also inhibits the neurotoxic action of β-amyloid and blocking L-type calcium channels, inhibits NMDA-type
glutamate receptors, and prevents mitochondrial leakage
10011349
Dimebolin (hydrochloride)
The hydrochloride form of Dimebolin soluble in both aqueous and organic solvents
13197
DAPT
An inhibitor of γ-secretase; blocks production of total Aβ in human primary neuronal cultures
10007963
E-64
A natural, potent, and irreversible inhibitor of cysteine proteases
10009021
AVE-1625
A highly potent, selective antagonist for the CB1 receptor; significantly improves the performance of rodents in working memory tasks
13033
Valproic Acid (sodium salt)
An inhibitor of histone deacetylases and GSK3 that depletes cellular inositol-1,4,5-trisphosphate; shows promise in combination therapy for
cancer and in treating Alzheimer’s disease
MAR2011
Cayman Chemical Ann Arbor, MI (800) 364-9897 caymanchem.com