For research use only. Not for therapeutic Use.
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM[1][3].
LY456236 (2 μM; 30 min) reduces DHPG (HY-12598A)-stimulated OCCM-30 proliferation[2].
LY456236 shows anticonvulsant effects in mice (3-100 mg/kg; i.p.; once) and rats (10-60 mg/kg; oral; once)[3].
| Catalog Number | R042522 |
| CAS Number | 338736-46-2 |
| Synonyms | 6-methoxy-N-(4-methoxyphenyl)quinazolin-4-amine;hydrochloride |
| Molecular Formula | C16H16ClN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H15N3O2.ClH/c1-20-12-5-3-11(4-6-12)19-16-14-9-13(21-2)7-8-15(14)17-10-18-16;/h3-10H,1-2H3,(H,17,18,19);1H |
| InChIKey | AVKFOWUSTVWZQN-UHFFFAOYSA-N |
| SMILES | COC1=CC=C(C=C1)NC2=NC=NC3=C2C=C(C=C3)OC.Cl |
| Reference | [1]. Ravikumar B, et al. Chemogenomic Analysis of the Druggable Kinome and Its Application to Repositioning and Lead Identification Studies. Cell Chem Biol. 2019 Nov 21;26(11):1608-1622.e6. [2]. Kanaya S, et al. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. [3]. Shannon HE, et al. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95. |
