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338736-46-2

338736-46-2 structure
338736-46-2 structure
  • Name: LY 456236
  • Chemical Name: 6-Methoxy-N-(4-methoxyphenyl)-4-quinazolinamine hydrochloride (1: 1)
  • CAS Number: 338736-46-2
  • Molecular Formula: C16H16ClN3O2
  • Molecular Weight: 317.770
  • Catalog: Signaling Pathways GPCR/G Protein mGluR
  • Create Date: 2017-09-19 17:37:19
  • Modify Date: 2025-08-25 15:26:26
  • 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].

Name 6-Methoxy-N-(4-methoxyphenyl)-4-quinazolinamine hydrochloride (1: 1)
Synonyms 6-Methoxy-N-(4-methoxyphenyl)-4-quinazolinamine hydrochloride (1:1)
(4-methoxy-phenyl)-(6-methoxy-quinazolin-4-yl)-amine HCl
6-Methoxy-N-(4-methoxyphenyl)quinazolin-4-amine hydrochloride (1:1)
4-Quinazolinamine, 6-methoxy-N-(4-methoxyphenyl)-, hydrochloride (1:1)
Description 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].
Related Catalog
Target

IC50: 0.145 μM (mGlu1), 0.91 μM (EGFR)[1]

In Vitro LY456236 (2 μM; 30 min) 降低 DHPG (HY-12598A) 刺激的 OCCM-30 增殖[2]。 Cell Proliferation Assay[2] Cell Line: OCCM-30 cells Concentration: 2 μM Incubation Time: 30 min, followed by 72 h incubation with DHPG (HY-12598A) Result: Reduced DHPG-stimulated OCCM-30 proliferation.
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: DBA/2 mice and CD1 mice, seizure models[3] Dosage: 3-100 mg/kg Administration: IP, once Result: Produced dose-related anticonvulsant effects in preventing audiogenic-induced (tonic-clonic) seizures in DBA/2 mice, threshold electroshock-induced seizures in CD1 mice, and 6 Hz electroshock-induced seizures in CD1 mice. Animal Model: Amygdala-kindled Sprague-Dawley rats[3] Dosage: 10, 30 and 60 mg/kg Administration: Oral, once Result: Produced dose-related decreases in behavioral and electrographic seizures at threshold stimulus intensity. Produced a dose-related increase in the stimulus intensity required to produce generalized seizures.
References

[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.  

Molecular Formula C16H16ClN3O2
Molecular Weight 317.770
Exact Mass 317.093109
PSA 56.27000
LogP 4.26560
Storage condition 2-8°C
Symbol GHS05 GHS07
GHS05, GHS07
Signal Word Danger
Hazard Statements H302-H315-H318-H335-H413
Precautionary Statements P261-P280-P305 + P351 + P338
Hazard Codes Xi
Risk Phrases 37/38-41
Safety Phrases 26-39
RIDADR NONH for all modes of transport
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