LY3020371 hydrochloride (C007B-364668)

LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor ( mGlu2/3 ) antagonist with K i of 5.3 and 2.5 nM, potently blocks cAMP formation with IC 50 of 16.2 nM LY3020371 hydrochloride exerts an antidepressant-like signature in vivo .In VitroLY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [ 3 H]-459477 with high affinity (hmGlu2 K i =5.26 nM; hmGlu3 K i =2.50 nM). LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC 50 =16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC 50 =6.21 nM). LY3020371 hydrochloride (LY3020371.HCl) blocks agonist-suppressed spontaneous Ca 2+ oscillations (IC 50 =34 nM) and in an intact hippocampal slice preparation (IC 50 =46 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoLY3020371 hydrochloride (LY3020371.HCl) (Intravenous injection; 3-15 mg/kg) in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors . LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10 mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:mGluR2 5.3 nM (Ki) mGluR3 2.5 nM (Ki). Specification: 0.99 Molecular Formula: C15H16ClF2NO5S Molecular Weight: 395.81 PubChem CID: 69669746 Isomeric SMILES: C1=CC(=C(C=C1SC[C@@H]2[C@H]([C@H]3[C@@H]([C@H]3[C@@]2(C(=O)O)N)C(=O)O)O)F)F.Cl

UPC:

51292806

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

L649210-5mg

CAS:

1377615-44-5

Product Size:

5mg