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Certificate of Analysis

  • Bioassay Tested

GABA(A) Receptor Modulator Explorer Kit

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

Cat #: EK-360
Size: 12 Vials
Form: Lyophilized

α-Asarone Cat #: A-260

Size: 1 g Source: Natural MW: 208.3 Purity: >99%
Origin
Acorus tatarinowii.
Effective concentration
1-500 µM.
Activity
α-Asarone 100 μM to 1 mM inhibits NaV1.2 channel currents. It also blocks GABA(A) receptors in neurons1. α-Asarone blocks corticosterone-induced anxiety-like behaviours via modulating TrkB signaling process2.
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 (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or three months at -20°C.

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.

Amentoflavone Cat #: A-165

Size: 1 mg Source: Natural MW: 538.46 Purity: ≥98.5%
Origin
Selaginella tamariscina.
Effective concentration
0.5 nM – 0.5 µM.
Activity
Amentoflavone is a negative allosteric modulator of GABA(A) receptor inhibitory activity, with EC50=4 µM on recombinant α1β2γ2L GABA(A) in oocytes1. In vitro, it potently displaces benzodiazepine binding to rat brain membranes with nM affinity2, and inhibits binding at other GPCRs3.
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 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.

(+)-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.

Bilobalide Cat #: B-145

Size: 10 mg Source: Natural MW: 326.3 Purity: >99.5%
Origin
Ginkgo biloba.
Effective concentration
1-100 µM.
Activity
Bilobalide is a 5-HT3A1 and GABAA2 channel blocker.
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 (10000 x g 5 min).
Storage after reconstitution
Up to four weeks at 4°C or 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.

Ganaxolone Cat #: G-120

Size: 5 mg Source: Synthetic MW: 332.5 Purity: ≥99%
Effective concentration
0.01-10 μM.
Activity
Ganaxolone potentiates GABA-evoked chloride currents. In Xenopus oocytes expressing the human GABA(A) receptor subunits α2β1γ2L, α3β1γ2L and α1β1γ2L the respective EC50 values are 94, 122 and 213 nM1. It is also used as an anticonvulsant, antiepileptic drug2.
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 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.

Muscimol hydrobromide Cat #: M-240

Size: 5 mg Source: Synthetic MW: 195.01 Purity: >96% (HPLC)
Effective concentration
0.01-1 µM.
Activity
Muscimol is a potent GABAA receptor agonist (EC50 of 0.92, 0.62 and 0.20 µM on α1/β3/γ2, α4/β3/γ2 and α4/β3/δ, respectively)1. It is also a partial agonist at GABAA-ρ receptor (EC50 of 3 µM on human homopentameric ρ1 receptor)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
Up to 200 mM 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.

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.

SJM-3 Cat #: S-215

Size: 5 mg Source: Synthetic MW: 354.4 Purity: >97%
Effective concentration
1-100 µM.
Activity
SJM-3 is a novel positive allosteric modulator of GABA(A) receptors at the benzodiazepine modulatory site (pKi = 6.7), strongly potentiating GABA currents at 30 µM via the binding site for diazepam in the transmembrane domain, while acting as an antagonist at the α+/γ− site1.
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 handling (10000 x g, 5 min).
Storage after reconstitution
-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.

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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