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LY 3130481

Chemical Structure : LY 3130481

CAS No.: 1610802-47-5

LY 3130481 (LY3130481;LY-3130481;CERC-611;CERC611)

Catalog No.: PC-60899Not For Human Use, Lab Use Only.

LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LY3130481 (CERC611) is a potent, selective, noncompetitive TARP γ8-associated AMPA receptors antagonist with IC50 of 65.3 nM (GluA1/TARP γ-8), with no activity for γ-2 (cerebellum) or other TARP members.
LY3130481 (CERC611) demonstrates fully protective against pentylenetetrazole-induced convulsions in rats without the motor impairment associated with non-TARP-dependent AMPA receptor antagonists.

Physicochemical Properties

M.Wt 382.438
Formula C19H18N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-6-(1-(1-(5-(2-hydroxyethoxy)pyridin-2-yl)-1H-pyrazol-3-yl)ethyl)benzo[d]thiazol-2(3H)-one

References

1. Gardinier KM, et al. J Med Chem. 2016 May 26;59(10):4753-68.

2. Kato AS, et al. Nat Med. 2016 Dec;22(12):1496-1501.

3. Witkin JM, et al. Neuropharmacology. 2017 Nov;126:257-270.

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