LY456236_product_DataBase

Bioactivity

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].

Target

IC50: 0.145 μM (mGlu1), 0.91 μM (EGFR)

Invitro

LY456236 (2 μM; 30 min) 降低 DHPG (HY-12598A) 刺激的 OCCM-30 增殖[2]。 Cell Proliferation Assay[2] Cell Line:

In Vivo

LY456236 在小鼠 (3-100 mg/kg; i.p.; once) 和大鼠 (10-60 mg/kg; oral; once) 中显示抗惊厥作用。 Animal Model:

Name

LY456236

CAS

338736-46-2

Formula

C16H16ClN3O2

Molar Mass

317.77

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

LY456236

CAS: 338736-46-2 F: C16H16ClN3O2 W: 317.77