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Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks | |
100 mg | Inquiry | 10-14 weeks |
Description | LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. |
Targets&IC50 | mGluR2:5.3 nM (ki), mGluR3:2.5 nM (ki) |
In vitro | LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC50=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC50=6.21 nM)[1]. LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM)[1].LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity (hmGlu2 Ki=5.26 nM;?hmGlu3 Ki=2.50 nM)[1]. |
In vivo | LY3020371 hydrochloride (LY3020371) administered via intraperitoneal injection at doses of 3 mg/kg and 10 mg/kg, 2 hours prior, significantly promotes wakefulness, notably decreasing NREM sleep in Wistar rats during the light phase[3]. Intravenous administration of LY3020371 hydrochloride at a dosage range of 3-15 mg/kg in rats results in cerebrospinal fluid concentrations predicted to efficiently inhibit mGlu2/3 receptors[1]. |
Molecular Weight | 395.81 |
Formula | C15H16ClF2NO5S |
Cas No. | 1377615-44-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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