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Certificate of Analysis

  • Bioassay Tested

Classical Ion Channel Blockers for Pain Research Explorer Kit

A Screening Package of Classical Ion Channel Blockers for Pain Research Economically Priced

Cat #: EK-355
Size: 24 Vials
Form: Lyophilized

α-Bungarotoxin Cat #: B-100

Size: 0.5 mg MW: 7984 Da Purity: >99% (HPLC) Net peptide content: 100%
Origin
Natural peptide isolated from Bungarus multicinctus (Many-banded krait).
Effective concentration
1 nM - 3 μM.
Activity
α-Bungarotoxin blocks postsynaptic neuromuscular transmission via competitive inhibition of nicotinic ACh receptors (nAChRs), thereby preventing the depolarizing action on postsynaptic membranes and blocking neuromuscular transmission. Selective for α7 receptors (IC50 value of 1.6 nM) and α3/β4 receptors (IC50 value of >3 μM)1,2. The toxin also blocks GABA(A) receptor subtypes3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or three months at -20°C.

α-Dendrotoxin Cat #: D-350

Size: 50 µg MW: 7048 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Natural peptide isolated from Dendroaspis angusticeps (Eastern green mamba).
Effective concentration
10-500 nM.
Activity
α-Dendrotoxin inhibits 4-AP sensitive, inactivating voltage-gated Kchannels (KV1.1, KV1.2 and KV1.6).
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

ω-Agatoxin IVA Cat #: STA-500

Size: 0.1 mg MW: 5202 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
20 nM - 1 µM.
Activity
ω-Agatoxin IVA is an antagonist of voltage-sensitive P-type Ca2+ channels1. It blocks neuromuscular transmission presynaptically in a variety of synapses2,3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any other aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or three months at -20°C.

ω-Conotoxin GVIA Cat #: C-300

Size: 0.1 mg MW: 3037 Da Purity: >99% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
20 nM - 1 μM.
Activity
ω-Conotoxin GVIA specifically and reversibly blocks N-type CaV channels1 and is reported to antagonize P2X receptors2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or three months at -20°C.

A-803467 Cat #: A-105

Size: 10 mg Source: Synthetic MW: 357.8 Purity: >99% (HPLC)
Effective concentration
10 nM - 10 μM.
Activity
A-803467 is a potent and selective blocker of the TTX-resistant NaV1.8 channel. A-803467 is a state dependent inhibitor with IC50 of 8 nM at depolarized membrane potential (-40 mV) and 80 nM at -100 mV. As an efficient inhibitor of TTX-resistant currents in DRG neurons, A-803467 was also effective as an analgesic in several rodent models of different pathological pain states1,2. A-803467 was used as a pharmacological tool to demonstrate the expression of NaV1.8 in the heart conduction system and its contribution to QRS interval in the mouse heart3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

A 967079 Cat #: A-225

Size: 5 mg Source: Synthetic MW: 207.2 Purity: >99% (HPLC)
Effective concentration
10 nM - 100 µM.
Activity
A 967079 is a blocker of TRPA1 channels and has IC50 values of 67 and 289 nM at human and rat TRPA1 receptors respectively1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 200 mM in DMSO. Centrifuge all product preparations before use (5,000 x g for 1 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

Apamin Cat #: STA-200

Size: 0.5 mg MW: 2028 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
100 nM - 1 µM.
Activity
Apamin is a blocker of voltage-independent Ca2+-activated K(SK) channels1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or two months at -20°C.

APETx2 Cat #: STA-160

Size: 0.1 mg MW: 4561 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
10 nM - 3 µM.
Activity
APETx2 inhibits ASIC3 channels1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to one week at 4°C or three months at -20°C.

(+)-Bicuculline Cat #: B-135

Size: 50 mg Source: Synthetic MW: 367.4 Purity: >99% (HPLC)
Effective concentration
1-100 µM.
Activity
(+)-Bicuculline inhibits (IC50 = 9 µM) recombinant α1β1γ2 GABA(A) channels that were activated with 3 µM GABA1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
DMSO (with gentle warming), DMF, chloroform. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

CNQX disodium salt Cat #: C-141

Size: 1 mg Source: Synthetic MW: 276.1 Purity: >98%
Effective concentration
300 nM - 500 µM.
Activity
AMPA/kainate receptor antagonist. The concentrations that inhibit 50% of AMPA binding (IC50) for CNQX in dorsal horn neurons and motoneurons are 300 nM-1.3 µM. It was about one-fifth as effective at kainate binding sites1,2. The association of AMPA receptors with TARPs converts CNQX from an antagonist to a weak partial agonist. CNQX binds with high affinity to both high and low affinity AMPA binding sites in rat brain. CNQX is a potent antagonist in electrophysiological responses mediated by non-NMDA receptors. Effects at NMDA receptors are much weaker.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C. Desiccation is recommended.
Reconstitution
Up to 20 mM in water. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
It is recommended to prepare stock solutions afresh whenever possible, and avoid long term storage. Otherwise, store in single use aliquots up to four weeks at 4°C or three months at -20°C.

Co 102862 Cat #: C-160

Size: 5 mg Source: Synthetic MW: 273.3 Purity: >96% (HPLC)
Effective concentration
0.1-200 μM
Activity
Co 102862 is a potent, broad spectrum and state-dependent blocker of neuronal voltage-gated Na+ channels that interacts selectively with inactivated states as opposed to resting states of the channel1. IC50 values are 0.28-15.9 µM in rat hippocampal neurons2. It is an anticonvulsant, demonstrating potent activity in rodent models of tonic/clonic and partial-complex seizures3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

D-AP5 Cat #: D-145

Size: 1 mg Source: Synthetic MW: 197.1 Purity: >95%
Effective concentration
100 nM - 100 µM.
Activity
D-AP5 is an NMDA receptor antagonist. IC50 = 0.28 µM (NR2A), 0.46 µM (NR2B), 1.6 µM (NR2C)1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
25 mg/ml in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

DNQX Cat #: D-131

Size: 10 mg Source: Synthetic MW: 252.1 Purity: >99%
Effective concentration
0.25-500 µM.
Activity
AMPA/kinate receptor antagonists. Association of AMPA receptors with TARPs converts DNQX from antagonist to weak partial agonist1. The concentration that inhibits 50% of AMPA binding (IC50) for DNQX is 0.50 ± 0.10 µM, and is about one-fifth as effective at kainate binding sites, 2.0 ± 0.1 uM in rat cortical membranes2. The IC50 of DNQX is 1 µM in a crystal structure of the GluR2 ligand binding core3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 40 mM in DMSO. Centrifuge before use (10000 x g, 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

Heteropodatoxin-2 Cat #: STH-340

Size: 0.1 mg MW: 3413 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
100-500 nM.
Activity
Heteropodatoxin-2 is an inhibitor of voltage-gated Kchannels of the KV4 family. Inhibition of KV4.3 and KV4.2 is strongly voltage-dependent, while inhibition of KV4.1 shows less voltage-dependence. Lacks affinity for KV1.4, KV2.1 and KV3.41,2. Also blocks Ca2+ channels1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to one week at 4°C or three months at -20°C.

Linopirdine dihydrochloride Cat #: L-156

Size: 5 mg Source: Synthetic MW: 464.39 Purity: >98%
Effective concentration
0.1-300 µM.
Activity
Linopirdine blocks KCNQ channels with an IC50 of 2.4 μM for KV7.2/3 heteromers1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
100 mM in water. Centrifuge all product preparations before use (10000 x g for 1 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

(+)-MK 801 maleate Cat #: M-230

Size: 5 mg Source: Synthetic MW: 337.4 Purity: >99% (HPLC)
Effective concentration
0.01-10 µM.
Activity
(+)-MK 801 maleate is a potent, selective and non-competitive NMDA receptor antagonist with an IC50 of 0.01 μM1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 100 mM in DMSO. Centrifuge all product preparations before use (5,000 x g for 1 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

NNC 55-0396 dihydrochloride Cat #: N-205

Size: 5 mg Source: Synthetic MW: 564.57 Purity: >95%
Effective concentration
1-100 µM.
Activity
NNC 55-0396 displays IC50 values of 6.8 and >100 μM for inhibition of CaV3.1 T-type channels and HVA currents respectively in INS-1 cells1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
50 mM in water. Centrifuge all product preparations before use (10000 x g for 1 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

NS8593 hydrochloride Cat #: N-195

Size: 5 mg Source: Synthetic MW: 299.79 Purity: >99%
Effective concentration
100 nM -10 µM.
Activity
NS8593 is KCa2 (SK) channel blocker, with no activity towards KCa3.1 channels, with IC50~100 nM1,2. It also blocks TRPM7 channels3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
50 mM DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

Phrixotoxin-1 Cat #: STP-700

Size: 50 µg MW: 3549 Da Purity: >99% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
10-100 nM.
Activity
Phrixotoxin-1 specifically and reversibly blocks KV4.2 and KV4.3 channels1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10,000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or three months at -20°C.

SB-705498 Cat #: S-160

Size: 5 mg Source: Synthetic MW: 428.05 Purity: >99%
Effective concentration
10 nM - 50 µM.
Activity
SB-705498 is a potent orally active TRPV1 blocker1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
DMSO 100 mM. Centrifuge all product preparations before use (10000 x g 1 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

SNX-482 Cat #: RTS-500

Size: 50 µg MW: 4495 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Recombinant, E. coli
Effective concentration
10-100 nM.
Activity
SNX-482 blocks R-type (CaV2.3) and P/Q-type (CaV2.1) voltage-gated Ca2+ channels1. It also blocks A-type K+ channels with an IC50 < 3 nM2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

Tertiapin Cat #: STT-250

Size: 0.1 mg MW: 2455 Da Purity: >98% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
10-100 nM.
Activity
Tertiapin blocks a range of inward rectifier K+ channels (Kir) in particular ROMK1 and GIRK but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine induced K+ currents in the heart2,3.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or three months at -20°C.

Waglerin-1 Cat #: STW-001

Size: 1 mg MW: 2520 Da Purity: >99% (HPLC) Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
1- 5 µM.
Activity
Waglerin-1 blocks ε subunit of muscle adult nAChR and modulates rodent GABA(A)/GABRA1 receptors1,2.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Any other aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to two weeks at 4°C or three months at -20°C.

XE991 dihydrochloride Cat #: X-101

Size: 5 mg Source: Synthetic MW: 449.37 Purity: >98%
Effective concentration
0.1-300 µM.
Activity
XE991 blocks KCNQ channels with IC50 of 0.5-10 µM1.
Storage before reconstitution
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Up to 50mM in water. Mild warming or agitation may be required. Spin-down all product preparations before handling.
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

For more information, please refer to individual certificate of analysis for each product.

For research purposes only, not for human use
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