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Certificate of Analysis

  • Bioassay Tested

GABA(A) Receptor Antagonist Explorer Kit

A Screening Package of GABA(A) Receptor Antagonists Economically Priced

Cat #: EK-420
Size: 11 Vials

(-)-Bicuculline methiodide Cat #: B-136

Size: 5 mg Source: Synthetic MW: 509.27 Purity: >96% (HPLC)
Effective concentration
0.1-10 µM.
Activity
(-)-Bicuculline methiodide is a water soluble quaternary salt of Bicucculine, a competitive antagonist of the GABAA receptors (IC50 = 8.4 µM)1. Quaternary salts of Bicucculine were shown to have effects not mediated by GABA 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 +4°C.
Reconstitution
Up to 20 mM in water. Also soluble in DMSO and ethanol. Centrifuge all product preparations before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

(-)-Bicuculline methochloride Cat #: B-137

Size: 5 mg Source: Synthetic MW: 417.84 Purity: >97% (HPLC)
Effective concentration
1-10 µM.
Activity
(-)-Bicuculline methochloride is a water soluble quaternary salt of Bicuculline, a competitive antagonist of the GABAA receptors (IC50 = 8.4 µM)1. Quaternary salts of Bicuculline were shown to have effects not mediated by GABA 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 +4°C.
Reconstitution
Soluble in water. Centrifuge all product preparations before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

Etbicyphat Cat #: E-175

Size: 50 mg Source: Synthetic MW: 178.12 Purity: >98%
Effective concentration
0.5-50 µM.
Activity
Etbicyphat, an ethyl bicyclophosphate organophosphorous compound, is a GABA receptor antagonist (KB = 3.98 µM for GABA(A) receptors),1 a blocker of neuronal voltage and GABA dependent Cl- currents, and a potent convulsant (≥0.4 mg/kg IP in rats) 2,3.
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
Soluble in water. Centrifuge before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

GABA(A)-Compound 1b Cat #: CMG-004

Size: 5 mg Source: Synthetic MW: 415.39 Purity: >98% (HPLC)
Effective concentration
0.1-10 µM.
Activity
A novel antagonist of α5 containing GABA(A) receptors, displaying significant selectivity for α5 (IC50 = 201 nM, Imax = 92%) over α1, α2, α3 and α4 containing receptors, on which it produces only partial maximum inhibition (Imax = 54, 0, 39 and 35%, respectively) at higher concentrations (IC50 = 0.48, >10, 0.48 and 0.91 µM, respectively)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
Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

Gabazine Cat #: G-215

Size: 5 mg Source: Synthetic MW: 287.32 Purity: >98% (HPLC)
Effective concentration
0.1-10 µM.
Activity
Gabazine is a competitive antagonist of the GABA(A) receptor, selectively inhibiting GABA-evoked currents (IC50 = 0.44 µM), but not currents evoked by pentobarbiton and etomidate1. It is also a low-affinity glycine receptor antagonist (KB = 191 µM)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
Soluble in methanol. Centrifuge all product preparations before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

Gabazine hydrobromide Cat #: G-216

Size: 5 mg Source: Synthetic MW: 368.23 Purity: >99% (HPLC)
Effective concentration
0.1-1 µM.
Activity
Gabazine is a competitive antagonist of the GABA(A) receptor, selectively inhibiting GABA-evoked currents (IC50 = 0.44 µM), but not currents evoked by pentobarbiton and etomidate1. It is also a low-affinity glycine receptor antagonist (KB = 191 µM)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
Soluble in water, DMSO and methanol. Centrifuge all product preparations before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

Oroxylin A Cat #: O-160

Size: 5 mg Source: Natural MW: 284.26 Purity: >98% (HPLC)
Origin
Scutellaria baicalensis.
Effective concentration
10 nM – 10 µM.
Activity
A flavonoid antagonist at the benzodiazepine site of the GABAA receptors. Inhibits [3H]Flunitrazepam binding to rat cerebral cortical membranes (IC50 = 1.09 µM), and selectively abolishes the anxiolytic, myorelaxant and motor incoordination, but not the sedative and anticonvulsant effects elicited by diazepam in mice1.
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 4°C. Keep in a tightly sealed container to protect from air. Protect from light.
Reconstitution
Up to 50 mM in DMSO. 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 product for storage.

Picrotoxin Cat #: P-325

Size: 500 mg Source: Natural MW: 602.58 Purity: >99% (HPLC)
Origin
Anamirta cocculus.
Effective concentration
1-100 µM.
Activity
Picrotoxin, an equimolar mixture of picrotoxinin and picrotin, is a non-competitive antagonist of the GABA(A) receptors (IC50 = 2.4 µM – 17 µM)1, an antagonist of glycine receptors (IC50 = 2.7 µM – 6.4 µM)2 and of 5-HT3 receptors (IC50 = 41.2 µM)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 +4°C.
Reconstitution
Soluble in DMSO and ethanol. Centrifuge before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

Tracazolate hydrochloride Cat #: T-230

Size: 5 mg Source: Synthetic MW: 340.85 Purity: >99%
Effective concentration
10-100 µM.
Activity
Tracazolate is an allosteric modulator of GABA(A) receptors, that was shown to potentiate (EC50 = 1.1-16.7 µM) or inhibit (IC50 = 1.2-4.0 µM) GABA-evoked currents in a subunit combination dependent manner1.
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 desiccated at -20°C. Protect from light.
Reconstitution
Soluble in 1eq. HCl and in 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.

U 93631 Cat #: U-120

Size: 5 mg Source: Synthetic MW: 299.37 Purity: >99%
Effective concentration
1-10 µM.
Activity
U 93631 is a ligand at the picrotoxin site of GABA(A) receptors, allosterically antagonizing GABA-induced Cl- currents by decreasing single-channel open probability1 and accelerating current decay (Kd = 2 µM)2. It is also an antagonist of 5-HT3A receptors (IC50 = 50 µM)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
Soluble in DMSO. Centrifuge before use (10000 x g, 5 min).
Storage after reconstitution
Up to 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.

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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