Certificate of Analysis

AMPA Receptor Antagonist Explorer Kit

A Screening Package of AMPA Receptor Antagonists Economically Priced
Cat #: EK-210 15 Vials

CNQX Cat #: C-140

Size: 5 mg Source: Synthetic MW: 232.2 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.
Reconstitution
DMSO. Centrifuge all product preparations before use (10000 x g for 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.

CP 465022 hydrochloride Cat #: C-335

Size: 5 mg Source: Synthetic MW: 499.4 Purity: >97% (HPLC)
Effective concentration
25 nM - 25 µM.
Activity
CP 465022 is a selective, non-competitive AMPA receptor antagonist. It inhibits AMPA receptor-mediated currents in rat cortical neurons (IC50 25 nM)1. It also partially blocks the persistent components of NaV1.6 channel activity2.
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 mM in DMSO. Centrifuge all product preparations before use.
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.

DNQX disodium salt Cat #: D-130

Size: 10 mg Source: Synthetic MW: 296.1 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
Water. 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.

Evans Blue tetrasodium salt Cat #: E-110

Size: 1 g Source: Synthetic MW: 960.8 Purity: >90%
Effective concentration
50 nM - 100 µM.
Activity
Evans Blue tetrasodium salt blocks glutamate receptors with IC50s 150 nM and 220 nM for kainate-type GluR6 and AMPA-type GluR11.
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
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.

GYKI 52466 hydrochloride Cat #: G-125

Size: 5 mg Source: Synthetic MW: 329.78 Purity: >96.6%
Effective concentration
300 nM - 300 µM.
Activity
GYKI 52466 is a selective allosteric AMPA/kainate receptor antagonist, with an IC50 of ~10 μM for AMPA induced currents in cultured superior colliculus neurons1.
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
30 mM in DMSO. 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.

Kynurenic acid Cat #: K-110

Size: 1 g Source: Synthetic MW: 189.2 Purity: >98%
Effective concentration
1 µM - 2 mM.
Activity
Kynurenic acid antagonizes ionotropic glutamate receptors with IC50 values of 33 µM (GluK2), 130 µM (GluK1). 100 µM - 3mM antagonizes NMDA response in rat spinal cord.
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 DMSO or in equimolar NaOH. Mild warming (37°C-42°C) and agitation may be required.
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

Naspm trihydrochloride Cat #: N-215

Size: 5 mg Source: Synthetic MW: 479.91 Purity: >95% (HPLC)
Effective concentration
300 nM - 10 µM.
Activity
Naspm trihydrochloride is a selective AMPA receptor antagonist; ~0.3 uM IC50 for AMPA induced currents in rat hipocampal neurons1.
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 H2O. 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.

NBQX Cat #: N-185

Size: 5 mg Source: Synthetic MW: 336.3 Purity: >99%
Effective concentration
0.1-500 µM.
Activity
NBQX is a potent inhibitor of non-NMDA glutamate receptor channels exhibiting IC50s of 0.1-0.4 μM for AMPA and 1.7-8 μM for kainate receptors1.
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.

NBQX disodium salt Cat #: N-186

Size: 1 mg Source: Synthetic MW: 380.2 Purity: >99%
Effective concentration
0.1- 500 µM.
Activity
NBQX is a potent inhibitor of non-NMDA glutamate receptor channels exhibiting IC50s of 0.1-0.4 μM for AMPA and 1.7-8 μM for kainate receptors1.
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
Water. 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.

PD-160725 2-hydroxyethanesulfonate Cat #: P-280

Size: 5 mg Source: Synthetic MW: 444.46 Purity: >98%
Effective concentration
0.1-100 µM.
Activity
PD-160725 2-hydroxyethanesulfonate is an AMPA receptor antagonist.
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 20 mM in H2O (slowly, clear yellow solution). Centrifuge all products before reconstitution (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C. It is recommended to aliquot reconstituted stock solutions.

PhTx-74 Cat #: P-120

Size: 1 mg Source: Synthetic MW: 507.54 Purity: >99% (HPLC)
Effective concentration
0.1-100 μM.
Activity
PhTx-74 (Philanthotoxin-7,4) is a synthetic polyamine analogue of the naturally occurring wasp venom toxin philanthotoxin-4,3,3. It is a potent and selective antagonist of certain isoforms of the AMPA type of ionotropic glutamate receptors1. PhTx-74 inhibited GluR1 and GluR3 homomers as well as GluR1/GluR2 where 100 μM inhibited nearly 100% of the glutamate evoked currents. However, up to 500 μM had no or little effect on GluR2 or GluR2/GluR3 channels1-2.
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
Water. Centrifuge all product preparations before use (10000 x g 5 min).
Storage after reconstitution
Up to one week at 4°C or six months at -20°C.

Talampanel Cat #: T-185

Size: 5 mg Source: Synthetic MW: 337.37 Purity: >97.8%
Effective concentration
10-300 µM.
Activity
Talampanel is a potent non-competitive AMPA/kainate receptor antagonist. It potentiates the anticonvulsive activity of antiepileptic drugs in animal models of seizures and is orally active1.
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 DMSO. Centrifuge all product preparations before use (10,000 x g for 1 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

YM 90K hydrochloride Cat #: Y-105

Size: 5 mg Source: Synthetic MW: 309.9 Purity: >99%
Effective concentration
50 nM - 50 µM.
Activity
YM 90K hydrochloride is a selective AMPA receptor antagonist; Ki of 84 nM1.
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
10 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 5 min).
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.