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BiochemicalTargets

Ions and other channels

Ion Channels are pore-forming proteins that allow the selective passage of ions through plasma or intracellular organelle membranes based on an electric gradient. In addition to transducing electrical currents in the body, they play a role in cellular signaling, pH regulation, and cell volume regulation. Ion channels can be defined by what opens and closes the channel: voltage-gated channels open and close based on the voltage gradient across the plasma membrane or ligand-gated channels by the binding of various ligands to the channel. They are also be defined by the type of ion that selectively passes through (calcium, sodium, potassium etc.) or by the physical stimulation that opens or closes them (mechanosensitive, light sensitive, or temperature sensitive). Many disease states are caused by perturbed ion channel function (channelopathies) including epilepsy, cystic fibrosis, long QT syndrome, and various musculo-skeletal disorders. Pharmacologic manipulation of ion channels is widely used to treat cardiovascular disorders, pain, diabetes, constipation and is being investigated for use in cancer, inflammation, immunomodulation, kidney diseases and infection.

AMPA

Domoic acid | Marine natural product neurotoxin

Domoic acid (DA; 14277-97-5)), a kainic acid-type neurotoxin produced by certain species of the marine pennate diatom Pseudo-nitzschia, is responsible for amnesic shellfish poisoning.1 Suspension feeders such as bivalve

Cyclothiazide | AMPA receptor positive allosteric modulator

CAS:
2259-96-3
Catalog Number:
10-2449
Activity:
AMPA receptor positiv e allosteric modulator
Chemical Name:
6-Chloro-3,4-dihydro-3-(5-norbornen-2-yl)-2H-1,2,4-benzothiadiazine-7-sulfonamide-1,1-dioxide
Alternate Names:
LY-35483
Molecular Weight:
389.88
Molecular Formula:
C14H16ClN3O4S2
Solubility:
Soluble in DMSO (up to 35 mg/ml) or in Ethanol (up to 9 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Aquaporins

AqB013 | Aquaporin blocker

AqB013 (1021869-51-1) is a selective aquaporin-1 and -4 inhibitor (IC50 ~ 20 mM) which acts at the cytoplasmic side of the AQP water pore.1 It blocks cGMP-stimulated human

TGN-020 | Aquaporin 4 blocker

CAS:
51987-99-6
Catalog Number:
10-1546
Activity:
Aquaporin 4 blocker
Chemical Name:
N-1,3,4-Thiadiazol-2-yl-3-pyridinecarboxamide
Molecular Weight:
206.22
Molecular Formula:
C8H6N4OS
Solubility:
Soluble in DMSO (up to 10 mg/ml with warming)
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

CVPA | Aquaporin 1 inhibitor

CAS:
37710-81-9
Catalog Number:
10-1430
Activity:
Aquaporin 1 inhibitor
Alternate Names:
3,3′-(1,3-Phenylene)bis(2-propenoic acid)
Chemical Name:
3-[3-(2-Carboxy-vinyl)-phenyl]-acrylic acid
Molecular Weight:
218.21
Molecular Formula:
C12H10O4
Solubility:
Soluble in DMSO (up to 25 mg/ml).
Physical Properties:
White solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of pruchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Calcium

YM-58483 | CRAC channel blocker

CAS:
223499-30-7
Catalog Number:
10-2935
Activity:
CRAC channel blocker
Chemical Names:
N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide
Alternate Name:
BTP2
Molecular Weight:
421.32
Molecular Formula:
C15H9F6N5OS
Solubility:
Soluble in DMSO (40 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Manidipine dihydrochloride | Calcium channel blocker

CAS:
89226-75-5
Catalog Number:
10-2045
Activity:
Calcium channel blocker
Chemical Names:
5-O-[2-(4-Benzhydrylpiperazin-1-yl)ethyl] 3-O-methyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate dihydrochloride
Alternate Name:
CV-4093
Molecular Weight:
683.63
Molecular Formula:
C35H38N4O6·2HCl
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
Room temperature
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Ionomycin Ca | Calcium Ionophore

CAS:
56092-82-1
Catalog Number:
10-2078
Activity:
Calcium ionophore
Fermentation product from:
Streptomyces conglobatus
Molecular Weight:
747.07
Molecular Formula:
C41H70O9·Ca
Solubility:
Soluble in DMSO (10 mg/ml); Ethanol (30 mg/ml)
Physical Properties:
White solid
Purity:
99% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Chloride

Glyburide | K-ATP channel blocker

CAS:
10238-21-8
Catalog Number:
10-1325
Activity:
K-ATP channel blocker
Alternate Names:
Glibenclamide
Chemical Name:
5-Chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]suphonyl]phenyl]ethyl]-2-methoxybenzamide
Molecular Weight:
494.01
Molecular Formula:
C23H28ClN3O5S
Solubility:
Soluble in DMSO (up to 45 mg/ml) or in Ethanol (up to 2 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

GABAA

Gaboxadol HCl | GABA-A receptor agonist

CAS:
64603-91-4
Catalog Number:
10-1168
Activity:
GABA-A receptor agonist
Alternate Names:
THIP HCl
Chemical Name:
4,5,6,7-Tetrahydroisoxazolo[5,4-c]pyridine-3-ol hydrochloride
Molecular Weight:
176.6
Molecular Formula:
C6H8N2O2 HCl
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 20 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Ionophores

Cereulide | Mitochondrial toxin

CAS:
157232-64-9
Catalog Number:
10-2746
Activity:
Mitochondrial toxin
Source:
Isolated from Bacillus cereus
Molecular Weight:
1153.40
Molecular Formula:
C57H96N6O16
Solubility:
Soluble in DMSO or Ethanol
Supplier As:
Supplied in Methanol at a concentration of 25μg/500μl
Purity:
98% by HPLC
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Diluted solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Salinomycin Na | Cancer stem cell inhibitor

CAS:
55721-31-8
Catalog Number:
10-2654
Activity:
Cancer stem cell inhibitor
Chemical Name:
from Streptomyces albus
Molecular Weight:
772.98
Molecular Formula:
C42H69O11 Na
Solubility:
Soluble in DMSO.
Physical Properties:
White solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Valinomycin | Induces loss of mitochondrial membrane potential

CAS:
2001-95-8
Catalog Number:
10-2112
Activity:
Induces loss of mitochondrial membrane potential
Chemical Name:
Cyclo(L-Val-D-HyIva-D-Val-L-Lac-)3
Molecular Weight:
1111.35
Molecular Formula:
C54H90N6O18
Solubility:
Soluble in DMSO (up to 10 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

Kainate

Domoic acid | Marine natural product neurotoxin

Domoic acid (DA; 14277-97-5)), a kainic acid-type neurotoxin produced by certain species of the marine pennate diatom Pseudo-nitzschia, is responsible for amnesic shellfish poisoning.1 Suspension feeders such as bivalve

Kainic acid | Kainate receptor agonist/neurotoxin

CAS:
487-79-6
Catalog Number:
10-2453
Activity:
Kainate receptor agonist; neurotoxin
Chemical Name:
(2S,3S,4S)-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid, hydrate
Molecular Weight:
213.24
Molecular Formula:
C10H15NO4 (xH2O)
Solubility:
Soluble in Water (up to 10 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20° for up to 3 months.
Shipping Code:
RT

nAChR

PNU 282987 | nAChR agonist

CAS Number:
123464-89-1
Catalog Number:
10-4496
Activity:
nAChR agonist
Chemical Name:
N-(3R)-1-Azabicyclo[2.2.2}oct-3-yl-4-chlorobenzamide
Molecular Weight:
264.75
Molecular Formula:
C14H17ClN2O
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

NMDA

Huperzine A | Acetylcholinesterase Inhibitor

Huperzine A (102518-79-6) is a nootropic alkaloid from the club moss Huperzia serrata that reversibly inhibits acetylcholinesterase (AChE, preferentially the tetrameric form, Ki = 7 nM)1, and antagonizes NMDA receptors

Flupirtine maleate | K+ channel activator

CAS:
75507-68-5
Catalog Number:
10-2416
Activity:
K+ channel activator
Chemical Name:
N-[2-Amino-6-[[(4-fluorophenyl)methyl]amino]-3-pyridinyl]carbamic acid ethyl ester maleate
Alternate Names:
D9998
Molecular Weight:
420.39
Molecular Formula:
C15H17FN4O2 • C4H4O4
Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 4 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Memantine HCl | NMDA antagonist / Anti-Alzheimer’s

CAS:
41100-52-1
Catalog Number:
10-2346
Activity:
NMDA antagonist / Anti-Alzheimer’s
Chemical Name:
3,5-Dimethyl-tricyclo[3.3.1.13,7]decam-1-amine HCl
Alternate Names:
3,5-Dimethyl-tricyclo[3.3.1.13,7]decam-1-amine HCl
Molecular Weight:
215.76
Molecular Formula:
C12H21N • HCl
Solubility:
Soluble in Water (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 2 months.
Shipping Code:
RT

P2X

BAY-1797 | P2X4 antagonist

CAS:
2055602-83-8
Catalog Number:
10-3980
Activity:
P2X4 antagonist
Chemical Names:
N-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide
Molecular Weight:
416.88
Molecular Formula:
C20H17ClN2O4S
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Pale brown solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

A-438079 HCl | P2X7 antagonist

CAS:
899431-18-6
Catalog Number:
10-4063
Activity:
P2X7 antagonist
Chemical Names:
3-[5-(2,3-Dichlorophenyl)tetrazol-1-ylmethyl]pyridine hydrochloride
Molecular Weight:
342.61
Molecular Formula:
C13H9Cl2N5·HCl
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White to off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Potassium

Repaglinide | Kir6 blocker

Repaglinide (135062-02-1) is a blocker of the ATP-sensitive potassium channel Kir6 with hypoglycemic activity.1 Clinically useful antidiabetic agent. It displays 30-fold selectivity for pancreatic Kir6.2/SUR1 over

VU0810464 | Kir3 activator

VU0810464 (2126040-21-7) is a potent (Kir3.1/3.2; GIRK1/2 EC50 = 165 nM) activator of G protein-gated inwardly-rectifying potassium channels (Kir3; GIRK).1,2 Displays selectivity for Kir3.1/3.2 versus Kir3.1/3.4

VU0134992 | Kir4.1 Blocker

VU0134992 (755002-90-5) is a blocker of the inward rectifier potassium channel Kir4.1 (IC50 = 970 nM).1 It also inhibits Kir3.1/3.2, Kir3.1/3.4, and Kir4.2 with similar potency.

Sodium

ICA-121431 | Selective Sodium channel blocker

CAS:
313254-51-2
Catalog Number:
10-4085
Activity:
Selective Nav1.1/1.3 inhibitor
Chemical Names:
2,2-Diphenyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]acetamide
Molecular Weight:
449.54
Molecular Formula:
C23H19N3O3S2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Off-white to beige solid
Purity:
>98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

PF-05089771 | Selective Nav1.7 inhibitor

CAS:
1235403-62-9
Catalog Number:
10-3990
Activity:
Selective Nav1.7 channel blocker
Chemical Name:
4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide
Alternate Name:
PF771
Molecular Weight:
500.34
Molecular Formula:
C18H12Cl2FN5O3S2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Benzamil HCl | Sodium channel/transport blocker

CAS:
161804-20-2
Catalog Number:
10-4541
Activity:
Sodium channel/transporter blocker
Chemical Names:
N-(Benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride
Molecular Weight:
356.21
Molecular Formula:
C13H14ClN7O·HCl
Solubility:
Soluble in DMSO (>25 mg/ml); water (5 mg/mL)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or may be stored at -20°C for up to 3 months.
Shipping Code:
RT

TRP

GFB-8438 | Selective TRPC5 inhibitor

GFB-8438 (2304549-73-1) is a potent (IC50 = 180 nM Qpatch and 280 nM whole cells) and selective inhibitor of TRPC4 and 5.1 It displayed excellent selectivity

BI 749327 | Selective TRPC6 blocker

CAS:
2361241-23-6
Catalog Number:
10-4318
Activity:
Selective TRPC6 blocker
Chemical Names:
[4-(6-Aminopyridazin-3-yl)piperidin-1-yl]-[4-[4-(trifluoromethyl)phenoxy]phenyl]methanone
Molecular Weight:
442.44
Molecular Formula:
C23H21F3N4O2
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

SB-705498 | TRPV1 blocker

CAS:
501951-42-4
Catalog Number:
10-3985
Activity:
TRPV1 blocker
Chemical Names:
1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridine-2-yl]pyrrolidine-3-yl]urea
Molecular Weight:
429.24
Molecular Formula:
C17H16BrF3N4O
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Other

GFB-8438 | Selective TRPC5 inhibitor

GFB-8438 (2304549-73-1) is a potent (IC50 = 180 nM Qpatch and 280 nM whole cells) and selective inhibitor of TRPC4 and 5.1 It displayed excellent selectivity

Repaglinide | Kir6 blocker

Repaglinide (135062-02-1) is a blocker of the ATP-sensitive potassium channel Kir6 with hypoglycemic activity.1 Clinically useful antidiabetic agent. It displays 30-fold selectivity for pancreatic Kir6.2/SUR1 over

VU0810464 | Kir3 activator

VU0810464 (2126040-21-7) is a potent (Kir3.1/3.2; GIRK1/2 EC50 = 165 nM) activator of G protein-gated inwardly-rectifying potassium channels (Kir3; GIRK).1,2 Displays selectivity for Kir3.1/3.2 versus Kir3.1/3.4