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Certificate of Analysis

  • Bioassay Tested

GABA(A) Receptor Agonist Explorer Kit

A Screening Package of GABA(A) Receptor Agonists Economically Priced
Cat #: EK-425
Size: 16 Vials

2'MeO6MF Cat #: M-245

Size: 5 mg Source: Synthetic MW: 266.3 Purity: >95%
Effective concentration
10-100 µM.
Activity
2'MeO6MF is a GABAA receptor modulator, shown to potentiate the response to GABA (EC10) with EC50 ranging from 21 µM to 98 µM, depending on subunit combination, in Xenopus oocytes. Displays anxiolytic-like and sedative effects 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 -20°C.
Reconstitution
Soluble up to 100 mM in DMSO. Spin down all products before handling.
Storage after reconstitution
Store at -20°C for several months. It is recommended to aliquot stock solutions to avoid repeated thawing and freezing.

AA 29504 Cat #: A-370

Size: 5 mg Source: Synthetic MW: 327.43 Purity: >98%
Effective concentration
1-100 µM.
Activity
AA 29504 is a positive allosteric modulator of GABA(A) receptors, reducing the EC50 of GABA and gaboxadol at the α4β3δ and α1β3γ2S receptors in Xenopus oocytes at over 1 µM. AA 29504, a retigabine analogue, also exhibits some agonistic activity on KCNQ channels (EC50=9.6-13.5 µM)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 +4°C.
Reconstitution
Soluble in DMSO. Centrifuge all product preparations before use (10000 x g, 5 min).
Storage after reconstitution
Up to three months at -20°C.

CGS 20625 Cat #: C-390

Size: 5 mg Source: Synthetic MW: 309.36 Purity: >99%
Effective concentration
1-100 µM.
Activity
CGS 20625 acts as a partial agonist at GABA(A) receptors (EC50 = 11.2-23.7 µM)1. It is a potent and selective non-benzodiazepine ligand at the central benzodiazepine receptor (IC50 = 1.3 nM), with anxiolytic and anticonvulsant effects in vivo2.
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.

Chlormethiazole hydrochloride Cat #: C-360

Size: 50 mg Source: Synthetic MW: 198.11 Purity: >96%
Effective concentration
0.01-1 mM.
Activity
Chlormethiazole both directly activates GABAA receptors (at 0.3 – 1 mM), and potentiates GABA-induced activation at various GABAA receptor subtypes (with EC50 of 20 – 160 µM)1. It was also shown to potentiate glycine-induced currents in both bovine chromaffin cells and murine spinal neurons (at 100 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 desiccated 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. It is recommended to aliquot reconstituted product for storage.

Diazepam Cat #: D-215

Size: 50 mg Source: Synthetic MW: 284.74 Purity: >98%
Effective concentration
1 nM – 10 µM.
Activity
Diazepam is a positive allosteric modulator of GABAA receptors at the benzodiazepine site, shown to increase single channel conductance1. Potentiates GABA induced chloride current (EC50=10-8 M in frog pituitary melanotrophs)2. Displaces [3H]Flunitrazepam from synaptosomal membranes of rat cerebellum, striatum and spinal cord (pIC50 > 7.5)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. Keep tightly sealed to protect from contact with air.
Reconstitution
Up to 100 mM in DMSO, up to 25 mM in ethanol. 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.

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.

Isoguvacine hydrochloride Cat #: I-185

Size: 25 mg Source: Synthetic MW: 163.6 Purity: >99%
Effective concentration
0.1-10 µM.
Activity
Isoguvacine hydrochloride is a specific agonist of the GABA(A) receptors, with EC50 of 3.7–17.3 µM, depending on subunit composition1.
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 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.

Ivermectin Cat #: I-110

Size: 250 mg Source: Synthetic MW: 875.09 Purity: >96%
Effective concentration
30 nM - 10 µM.
Activity
Ivermectin is a positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor1 and the purinergic P2X4 receptor2. It also modulates glutamate- and GABA-activated chloride channels and potentiates glycine-gated currents at low concentrations (30 nM)3,4.
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.

Lorazepam Cat #: L-230

Size: 10 mg Source: Synthetic MW: 321.16 Purity: >99%
Effective concentration
1 nM – 10 µM.
Activity
Lorazepam is a positive allosteric modulator of GABA(A) receptors at the benzodiazepine site. It potentiates GABA-induced chloride currents at sub-micromolar concentrations1. It displaces [3H]Flunitrazepam from GABA(A) receptors in rat cerebral cortex (IC50 = 4.8 nM)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. Keep tightly sealed.
Reconstitution
Up to 100 mM in DMSO, up to 40 mM in ethanol. 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.

MmTx1 Toxin-ATTO Fluor-488 Cat #: STM-550-AG

Size: 5 µg MW: ~7775 Da. Purity: >99%. Net peptide content: 100%
Origin
Synthetic peptide
Effective concentration
200-400 nM.
Activity
MmTx1 is a potent allosteric modulator of GABA(A) receptors1.
Storage before reconstitution
Lyophilized powder 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.

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.

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.

Zaleplon Cat #: Z-140

Size: 10 mg Source: Synthetic MW: 305.34 Purity: >98%
Effective concentration
10 nM – 10 µM.
Activity
A non-benzodiazepine pyrazolopyrimidine agonist at the benzodiazepine site of the GABAA receptors. Potentiates GABA-induced chloride currents at sub-micromolar concentrations1. Displaces [3H]Flunitrazepam from rat cerebellum and spinal cord membranes with IC50 values of 167 nM and 2.38 µM, respectively2.
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 4°C.
Protect from light.
Reconstitution
Up to 100 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.

Zolpidem Cat #: Z-100

Size: 5 mg Source: Synthetic MW: 307.39 Purity: >99%
Effective concentration
0.1-100 nM.
Activity
GABA(A) receptor agonist at the benzodiazepine site, potent and highly selective for α1-subunit-containing receptors (EC50 = 47.8 nM on α1β1γ2L)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
Up to 100 mM in Ethanol and 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.

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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