ION CHANNEL MODULATORS
CALCIUM CHANNEL MODULATORS
CA-250
w-Agatoxin TK
Funnel web spider toxin
98% [145017-83-0] MW=5273 Storage: -20蚓
Caution! Highly toxic. Handle with care.
w-Agatoxin TK is a peptide toxin
from the funnel web spider Agelenopsis aperta. It is a selective blocker of the
P-type Ca2+channel (IC50=15 nM)12. It
also blocks a Q-type-like Ca2+ channel in rat hippocampal neurons with low
sensitivity3.
50 mg
5 x 50 mg
CA-200
Amiloride廈Cl
99%, MW=266.1 [2016-88-8] Storage: RT
In chick dorsal root ganglion and mouse neuroblastoma cells amiloride selectively blocks
the low threshold (T-type) calcium channel (KD=30 然) with no effect on L-type
channels or tetrodotoxin sensitive Na+ channels4.
It also inhibits the epithelial tetrodotoxin insensitive Na+ channel (IC50=1
然)5,6,7. It is a clinically useful K+ sparing
diuretic8.
1 g
5 g
CA-410
BAY K-8644
98%, MW=356.3 [98791-67-4] Storage: 0蚓
A potent, direct acting, voltage-sensitive Ca2+ channel activator9,10.
It exerts positive inotropic, vasoconstrictive and positive chronotropic activity (in
vitro and in vivo) in a concentration range from 10-9 to 10-7
M11.
5 mg
5 x 5 mg
CA-235
w-Conotoxin GVIA
99%, MW=3037 [92078-76-7] Storage: -20蚓
Caution! Highly toxic. Handle with care.
w-Conotoxin GVIA is a peptide toxin from the snail Conus
geographus12,13. It is a highly selective blocker of the
high voltage-activated (N-type) calcium channel14,15.
0.5 mg
5 x 0.5 mg
CA-255
w-Conotoxin MVIIC
99%, MW=2749 [147794-23-8] Storage: -20蚓
Caution! Highly toxic. Handle with care.
w-Conotoxin MVIIC is a peptide toxin from the snail Conus
magus. It blocks both N- and Q-type Ca2+channels at 10 然16.
Q-type channels are completely blocked at 1.5 然17
100 痢
5 x 100 痢
CA-205
Diltiazem廈Cl
99%, MW=451.0 [33286-22-5] Storage: RT
Selectively blocks the voltage-sensitive (L-type) calcium channel18,19.
1 g
5 g
CA-206
Dotarizine
99%, MW=442.6 [84625-59-2] Storage: RT
Blocks Ca2+ entry through Ca2+ channels. More potent in rabbit
basilar arteries than aorta20.
10 mg
50 mg
CA-225
Flunarizine?HCl
98%, MW=477.4 [30484-77-6] Storage: 0蚓
Flunarizine selectively blocks the low threshold (T-type) calcium channel in rat
hippocampal CA1 pyramidal neurons21. It inhibits Ca2+-influx-induced
vasoconstriction of peripheral and cerebral blood vessels with little effect on myogenic
activity and Ca2+-dependent myocardial contractility19,22.
1 g
5 g
CA-245
FPL-64176
98%, MW=347.4 [120934-96-5] Storage: -20蚓
A potent L-type Ca2+ channel opener23. Induces a
contractile response in cardiac and vascular smooth muscle, EC50=0.2 然24.
10 mg
50 mg
CA-240
Maitotoxin
>90%, MW=3424 [59392-53-9] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Maitotoxin is a non-peptide toxin isolated from the dinoflagellate Gambierdiscus
toxicus. It activates voltage-sensitive (L-type) calcium channels in a variety of
cells25,26. It also activates phosphoinositide turnover and
stimulates arachidonic acid metabolism at concentrations as low as 0.03-0.3 ng/ml27.
10 痢
CA-210
Nifedipine
99%, MW=364.3 [21829-25-4] Storage: RT
Selectively blocks the voltage-sensitive (L-type) calcium channel19,28.
1g
5 g
CA-211
Nimodipine
99%, MW=418.5 [66085-59-4] Storage: RT
A dihydropyridine-type voltage-sensitive (L-type) calcium channel blocker. Selectively
acts on the cerebral vasculature29. Blocks some low-voltage
activated Ca2+ channels30.
50 mg
250 mg
CA-212
Nitrendipine
99%, MW=360.4 [39562-70-4] Storage: RT
A dihydropyridine-type voltage-sensitive (L-type) calcium channel blocker. Modulates NMDA
receptor channel function in mammalian neurons31. Inhibits
neutrophil adhesion to vascular endothelium32.
50 mg
250 mg
CA-227
SDZ-202 791 R(-)
99%, 358.4 [97217-84-0] Storage: RT
A dihydropyridine-type voltage-sensitive (L-type) calcium channel blocker33,35.
1 mg
CA-226
SDZ-202 791 S(+)
99%, 358.4 [97217-84-0] Storage: RT
A dihydropyridine-type voltage-sensitive (L-type) calcium channel opener34,35.
At 10 然, it increased calcium channel current in voltage-clamped vascular smooth muscle
cells from rabbit ear artery36.
1 mg
CA-230
SK&F 96365
1-[b-[3-(4-Methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole廈Cl
98%, MW=402.9 [130495-35-1] Storage: RT
A novel, selective inhibitor of receptor-mediated calcium entry. It inhibits
receptor-mediated calcium entry in stimulated platelets (IC50=8-12 然)
neutrophils and endothelial cells at concentrations which do not affect internal Ca2+
release37,38,39. It also inhibits voltage-gated Ca2+ entry
in excitable cells37,40. Note, in some cells SK&F 96365
can activate a novel Ca2+ entry pathway41.
5 mg
25 mg
CA-260
Tetrandrine
98%, MW=622.8 [518-34-3] Storage: RT
Tetrandrine is a bis-coclaurine alkaloid which has been used for centuries in Chinese
traditional medicine for cardiovascular diseases42. It
blocks the L-type (IC50= 0.3-8 然) and T-type (IC50= 2.5-20 然)
calcium channels43. It is also a potent blocker of the Ca2+-activated
K+ channel (Kd= 0.2 然)44,74.
50 mg
250 mg
CA-215
Verapamil廈Cl
99%, MW=491.1 [23313-68-0] Storage: RT
Selectively blocks the slow voltage-sensitive (L-type) calcium channel19,45.
1 g
5 g
POTASSIUM CHANNEL MODULATORS
KC-150
Apamin
>95%, MW=2027 [24345-16-2] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Apamin is an octadecapeptide found in the venum of the honey bee (Apis mellifera).
It is a potent (1-10 nM) and highly selective inhibitor of the low conductance Ca2+-activated
K+ channel46,47,48.
500 痢
5 x 500 痢
KC-100
Charybdotoxin
>98%, MW=4295 [95751-30-7] Storage: -20蚓
Caution! Highly toxic. Handle with care.
A potent and selective inhibitor of the high conductance Ca2+-activated K+
channel49,50,51. It inhibits K+ conductance and
mitogen-stimulated proliferation (Ki=300 and 500 pM respectively) in human T
lymphocytes51,52.
100 痢
5 x 100 痢
KC-110
Dendrotoxin (from Dendroaspis angusticeps)
98%, MW=7030 [74811-93-1] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Dendrotoxin selectively inhibits voltage gated K+ channels. At nanomolar
concentrations it inhibits several types of outward K+ currents, particularly
the transient outward current (A-current). However A-channels vary greatly in their
sensitivity to dendrotoxin53,54,55,46
100 痢
5 x 100 痢
KC-115
Diazoxide
98%, MW=230.7 [364-98-7] Storage: RT
A selective ATP-sensitive K+ (KATP) channel opener56,57,58.
It is a well established antihypertensive/vasodilator59. It
opens KATP channels in pancreatic b-cells56.
1 g
5 g
KC-120
Glyburide (glibenclamide)
98%, MW=494.0 [10238-21-8] Storage: RT
An antidiabetic sulfonylurea which selectively blocks ATP-sensitive K+ channels60. It blocks vascular smooth muscle relaxation produced by KATP
channel openers61. High affinity binding sites are widely
distributed and have been identified in the cardiovascular system62,
the CNS63 and in pancreatic b-cells64. It displays a large potency difference in pancreatic tissue
(IC50 in the nM range) versus vascular tissue (IC50 in the 然
range)61.
1 g
5 g
HE-008
Hepoxilin A3
Hepoxilin A3 is an eicosanoid which is produced endogenously in a receptor
dependent process and opens IK(5-HT) (S-K+) channels in Aplysia
sensory cells (L14)65 and rat hippocampal CA1 neurons66. For reviews on eicosanoids in ion channel modulation and
signal transduction see references 67,68,69
KC-141
5-Hydroxydecanoate意a
98%, MW=210.3 [624-00-0] Storage: 0蚓
Inhibits ATP-sensitive K+ channels70.
100 mg
500 mg
KC-125
Minoxidil (U-10858)
98%, MW=209.3 [38304-91-5] Storage: RT
A selective ATP-sensitive K+ (KATP) channel opener71.
It is metabolized to the more active sulfate in vivo. A clinically useful
anti-alopecia72.
100 mg
500 mg
KC-130
Minoxidil sulfate (U-58838)
98%, MW=289.3 [83701-22-8] Storage: RT
A selective ATP-sensitive K+ (KATP) channel opener71.
It is the active metabolite of minoxidil and is a potent (IC50=0.14 然)
vascular smooth muscle relaxant61,72.
5 mg
25 mg
KC-155
Paxilline
98%, MW=435.6 [57186-25-1] Storage: -20蚓
Paxilline is an indole alkaloid isolated from Penicillium paxilli. It is a
selective and reversible blocker of the high conductance Ca2+-activated K+
(maxi-K) channel (70% block at 10nM)73,74
2 mg
5 mg
KC-156
Paxillinol
98%, MW=437.6, Storage: -20蚓
A negative control for the maxi-K channel inhibitor paxilline (50% block at 0.1-1 然)73.
1 mg
KC-131
PCO 400
99%, MW=299.3 [121055-10-5] Storage: RT
A potent and selective opener of ATP-sensitive K+ (KATP) channels75,76,77. For reviews on potassium channel openers, see
references78,79,80.
20 mg
100 mg
KC-157
Penitrem A
98%, MW=634.2 [12627-35-9] Storage: -20蚓
A selective, irreversible blocker of the high conductance Ca2+-activated K+
(maxi-K) channel (100% block at 10 nM)73.
1 mg
5 mg
KC-135
Tolazamide (U-17835)
98%, MW=311.4 [1156-19-0] Storage: RT
An antidiabetic sulfonylurea which selectively blocks ATP-sensitive K+ channels60.
2 g
10 g
KC-140
Valinomycin
99%, MW=1111.4 [2001-95-8] Storage: RT
A potassium ionophore. Antagonizes endothelin induced vasoconstriction (IC50=0.3
然)82.
25 mg
5 x 25 mg
SODIUM CHANNEL MODULATORS
CA-200
Amiloride廈Cl
Inhibits the epithelial tetrodotoxin insensitive Na+ channel (IC50=1
然)5,6,7.
NA-130
Brevetoxin PbTx-1
>95%, MW=866.6 [98112-41-5] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Voltage-dependent Na+ channel activator83.
100 痢
5 x 100 痢
NA-105
?Conotoxin GIIIB (Geographutoxin II)
98%, MW=2615 [140678-12-2] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Occurs in the venum of Conus geographus12. It is a
selective blocker of the voltage-dependent Na+ channel, interacting
competitively with saxitoxin and displaying high selectivity (>1,000-fold) for muscle
versus nerve Na+ channels13,84,85.
EC50s for blocking contraction of isolated rat and rabbit muscles are 60 nM and
50 nM respectively13.
500 痢
5 x 500 痢
NA-135
Grayanotoxin III
90%, MW=414.5 [4678-45-9] Storage: -20蚓
Sodium channel opener86.
1 mg
5 x 1 mg
A-248
Monensin意a
90-95%, MW=692.9 [22373-78-0] Storage: 4蚓
A Na+ ionophore. Inhibits protein secretion87.
Blocks ceramide transport through the Golgi88.
1 g
PE-165
Palytoxin
98%, MW=2677.4 [77734-91-9] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Palytoxin is a non-peptide toxin isolated from various species of the coelenterate Palythoa89. It is a potent activator of the tetrodotoxin-insensitive Na+
channel90. It stimulates catecholamine release from cultured
bovine adrenal chromaffin cells91 and stimulates arachidonic
acid metabolism 1000 to 3000 times greater than the TPA type tumor promoters92.
Though a potent tumor promoter, it does not compete for the TPA receptor93.
100 痢
5 x 100 痢
NA-115
Saxitoxin
99%, MW=299.3 [35523-89-8] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Saxitoxin is a non-peptide toxin isolated from Gonyaulax sp. It is a potent,
reversible inhibitor of the voltage-dependent Na+ channel94,95.
100 痢
5 x 100 痢
NA-116
SDZ-201106 (?, (DPI-201106)
99%, MW=466.6 [97730-95-5] Storage: RT
Sodium channel opener96. Positive inotropic agent97,98.
20 mg
100 mg
NA-117
SDZ-201106 (+)
99%, MW=466.6, Storage: RT
(+)-Enantiomer of sodium channel opener SDZ-201106.
5 mg
NA-118
SDZ-201106 (-)
99%, MW=466.6, Storage: RT
(-)-Enantiomer of sodium channel opener SDZ-201106.
5 mg
NA-120
Tetrodotoxin (from Fugu sp.)
98%, MW=319.3 [4368-28-9] Storage: -20蚓
Caution! Highly toxic. Handle with care.
Tetrodotoxin is a non-peptide toxin isolated from a variety of organisms99.
It is a potent, reversible inhibitor of the voltage-dependent Na+ channel94,95,100. In CHO cells transfected with cDNA
encoding the RIIA sodium channel a subunit from rat
brain, tetrodotoxin completely blocked the voltage-activated Na+ current at 200
nM101.
1 mg
5 x 1 mg
NA-125
Veratridine
98%, MW=673.8 [71-62-5] Storage: -20蚓
A Na+ channel activator. Veratridine acts at neurotoxin receptor site 2 and
preferentially binds to activated Na+ channels causing persistent activation.
It prevents inactivation and shifts activation to more negative potentials102,103,104,105.
10 mg
5 x 10 mg
CHLORIDE CHANNEL INHIBITORS
CM-101
IAA-94
R(+)-[(6,7-Dichloro-2-cyclopentyl-2,3-dihydro-2-methyl-1-oxo-1H-inden-5-yl)-oxy]acetic
acid
98%, MW=357.2 [54197-31-8] Storage: RT
A potent mammalian skeletal muscle106 and epithelial107,108 chloride channel blocker (Ki=1 然 in
bovine kidney cortex microsomes). May be used to assay, enrich and characterize skeletal
muscle chloride channels106.
10 mg
50 mg
CM-100
5-Nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB)
98%, MW=300.3 [107254-86-4] Storage: RT
A potent chloride channel blocker (IC50=0.1-100 然 depending on channel
subtype and assay method)109,110. Inhibits cyclooxygenase
(IC50=8 然)111.
10 mg
50 mg
ION PUMP REAGENTS
CM-110
Bafilomycin A1
>95%, MW=622.8 [88899-55-2] Storage: -20蚓
A potent and selective inhibitor of vacuolar ATPases (V-type), IC50=0.004-0.4
nmol/mg112. Blocks lysosomal cholesterol trafficking in
macrophages113. Blocks pH regulation in brain cells114. Useful tool for distinguishing different types of ATPases112.
100 痢
5 x 100 痢
EI-168
Bumetanide (Ro 10-6338)
98%, MW=364.4 [28395-03-1] Storage: RT
Bumetanide is a specific inhibitor of Na-K-2Cl cotransport115,116.
It binds specifically, saturably and with high affinity to membranes from a large variety
of cells117. A clinically useful diuretic.
1 g
5 g
CM-112
Clopamide
98%, MW=345.8 [636-54-4] Storage: RT
Clinically useful diuretic118.
500 mg
CM-111
Oligomycin A
98%, MW=791.1 [579-13-5] Storage: -20蚓
Inhibits mitochondrial ATPases (F1Fo)119.
Stimulates lysosome acidification due to shunting of membrane potential120.
5 mg
25 mg
Na+/K+ ATPase ANTIBODIES
SA-247
Anti-Na+/K+ ATPase, a-3 subunit
Mouse monoclonal antibody. Clone XVIF9-G10. Immunogen: Canine cardiac microsomes. Supplied
as IgG in ascites. Recognizes ~110 kDa a-3 subunit of the Na+/K+
ATPase. Cross-reacts with human, monkey, sheep, rabbit, dog and rat. Applications: WB 1
痢/ml, IH 5 痢/ml.
100 痢
SA-112
Anti-Na+/K+ ATPase
Mouse monoclonal antibody. Clone I05. Supplied as purified IgM, 1 mg/ml. Recognizes native
and denatured b (45 kDa) subunit of Na+/K+
ATPase. Cross-reacts with human, rabbit, dog, and other mammalian species. Applications:
WB, IF.
1 mg
SA-113
Anti-Na+/K+ ATPase
Chicken polyclonal antibody. Immunogen: Highly purified Na+/K+
ATPase (canine kidney). Supplied as purified IgG, 10 mg/ml. Recognizes the intact enzyme, a (100 kDa) and b (50 kDa) subunits,
glycosylated and non-glycosylated forms. Cross-reacts with other tissues and species.
Applications: WB 1/500, ELISA
10 mg
5 x 10 mg
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