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Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $293 | In Stock | |
5 mg | $722 | In Stock | |
10 mg | $987 | In Stock | |
25 mg | $1,520 | In Stock | |
50 mg | $1,980 | In Stock |
Description | Golexanolone (Golexanolona) is a novel GABA-A receptor-modulating steroid antagonist that reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in rats with chronic hyperammonemia, and may be used to study hepatic encephalopathy. |
In vitro | In the absence of agonist (i.e., GABA, 0), the THDOC-mediated outward current excursion was significantly reduced when Golexanolone(GR3027) concentration was incrementally increased (0.03-3 µM, Fig. 2A), with an IC50 = 344 nM and Imax -33%. In addition, analysis of the AUC and peak current amplitude of the GABA-mediated response showed a concentration-dependent decrease in both parameters (IC50 = 341 nM, Imax -35% for AUC; IC50 = 563 nM, Imax -37% for peak current amplitude; n = 4-14, 95% confidence intervals;) The data suggest that the effects of Golexanolone(GR3027) on the THDOC-mediated α5β3γ2L GABAA channel activation.[2] |
In vivo | In a toxicity study using doses of 50 and 100 mg/kg/day to evaluate oral administration of Golexanolone(GR3027) in rats, no toxicity was observed at 100 mg/kg/day.[1] |
Alias | GR-3027, Golexanolonum, Golexanolona |
Molecular Weight | 329.48 |
Formula | C21H31NO2 |
Cas No. | 2089238-18-4 |
Smiles | C[C@@]12[C@@]3([C@]([C@]4([C@](C)(CC3)\C(=N\O)\CC4)[H])(CC[C@]1(C[C@@](C#C)(O)CC2)[H])[H])[H] |
Relative Density. | 1.22 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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