LY456236 HCl | CAS# 338736-46-2 | 338738-57-1 | mGlu1 receptor antagonist

LY456236 HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532169

CAS#: 338736-46-2 (HCl)

Description: LY456236 is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively). LY456236 HCl reduces hyperalgesic behavior induced by formalin in both mouse and rat with ED50 values of 28 and 16.3 mg/kg respectively.

Chemical Structure

LY456236 HCl

CAS# 338736-46-2 (HCl)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 532169
Name: LY456236 HCl
CAS#: 338736-46-2 (HCl)
Chemical Formula: C16H16ClN3O2
Exact Mass: 0.00
Molecular Weight: 317.773
Elemental Analysis: C, 60.48; H, 5.08; Cl, 11.16; N, 13.22; O, 10.07

Price and Availability

Size	Price	Availability
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6150	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 338736-46-2 (HCl) 338738-57-1 (free base)

Synonym: LY456236 HCl; LY456236 Hydrochloride; LY456236 ; LY 456236 ; LY-456236.

IUPAC/Chemical Name: 6-Methoxy-N-(4-methoxyphenyl)-4-quinazolinamine hydrochloride

InChi Key: AVKFOWUSTVWZQN-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: COC1=CC=C(NC2=C3C=C(OC)C=CC3=NC=N2)C=C1.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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Product Data:

Product Data

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Biological target:	LY456236 HCl is a selective mGlu1 receptor antagonist (IC50 values are 143 nM and > 10 μM for mGlu1 and mGlu5 receptors respectively).
In vitro activity:	OCCM-30 cells, immortalized murine cementoblasts, were stimulated with l-glutamate or mGluRs antagonists. Dihydroxyphenylglycine (DHPG), an agonist of group I mGluRs (mGluR1 and mGluR5), also promoted cell proliferation, and this was inhibited by LY456236, an mGluR1 antagonist. DHPG increased the expression of cyclin D1, a key regulator of cell proliferation, and its nuclear translocation. Reference: Connect Tissue Res. 2016 Sep;57(5):417-26. https://pubmed.ncbi.nlm.nih.gov/27261070/
In vivo activity:	The purpose of the present experiments was to characterize the anticonvulsant effects of the selective mGlu1 receptor antagonist LY456236 in mice and rats. In male and female DBA/2 mice, LY456236 produced a dose-related inhibition of sound-induced clonic-tonic seizures. In male CF1 mice, LY456236 produced a dose-related inhibition of tonic extensor seizures in the threshold electroshock model, and limbic seizures in the 6-Hz focal seizure model. Reference: Neuropharmacology. 2005;49 Suppl 1:188-95. https://pubmed.ncbi.nlm.nih.gov/16011839/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	6.4	20.01

Preparing Stock Solutions

The following data is based on the product molecular weight 317.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Kanaya S, Komatsu H, Shimauchi H, Nemoto E. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. doi: 10.1080/03008207.2016.1195826. Epub 2016 Jun 3. PMID: 27261070. 2. Shannon HE, Peters SC, Kingston AE. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95. doi: 10.1016/j.neuropharm.2005.05.010. PMID: 16011839. 3. Barton ME, Shannon HE. Behavioral and convulsant effects of the (S) enantiomer of the group I metabotropic glutamate receptor agonist 3,5-DHPG in mice. Neuropharmacology. 2005 May;48(6):779-87. doi: 10.1016/j.neuropharm.2005.01.017. PMID: 15829250.
In vitro protocol:	1. Kanaya S, Komatsu H, Shimauchi H, Nemoto E. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. doi: 10.1080/03008207.2016.1195826. Epub 2016 Jun 3. PMID: 27261070.
In vivo protocol:	1. Shannon HE, Peters SC, Kingston AE. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95. doi: 10.1016/j.neuropharm.2005.05.010. PMID: 16011839. 2. Barton ME, Shannon HE. Behavioral and convulsant effects of the (S) enantiomer of the group I metabotropic glutamate receptor agonist 3,5-DHPG in mice. Neuropharmacology. 2005 May;48(6):779-87. doi: 10.1016/j.neuropharm.2005.01.017. PMID: 15829250.

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1: Kanaya S, Komatsu H, Shimauchi H, Nemoto E. Metabotropic glutamate receptor 1 promotes cementoblast proliferation via MAP kinase signaling pathways. Connect Tissue Res. 2016 Sep;57(5):417-26. doi: 10.1080/03008207.2016.1195826. PubMed PMID: 27261070.

2: Rorick-Kehn LM, Hart JC, McKinzie DL. Pharmacological characterization of stress-induced hyperthermia in DBA/2 mice using metabotropic and ionotropic glutamate receptor ligands. Psychopharmacology (Berl). 2005 Dec;183(2):226-40. PubMed PMID: 16175401.

3: Shannon HE, Peters SC, Kingston AE. Anticonvulsant effects of LY456236, a selective mGlu1 receptor antagonist. Neuropharmacology. 2005;49 Suppl 1:188-95. PubMed PMID: 16011839.

4: Barton ME, Shannon HE. Behavioral and convulsant effects of the (S) enantiomer of the group I metabotropic glutamate receptor agonist 3,5-DHPG in mice. Neuropharmacology. 2005 May;48(6):779-87. PubMed PMID: 15829250.

5: Varty GB, Grilli M, Forlani A, Fredduzzi S, Grzelak ME, Guthrie DH, Hodgson RA, Lu SX, Nicolussi E, Pond AJ, Parker EM, Hunter JC, Higgins GA, Reggiani A, Bertorelli R. The antinociceptive and anxiolytic-like effects of the metabotropic glutamate receptor 5 (mGluR5) antagonists, MPEP and MTEP, and the mGluR1 antagonist, LY456236, in rodents: a comparison of efficacy and side-effect profiles. Psychopharmacology (Berl). 2005 Apr;179(1):207-17. PubMed PMID: 15682298.

6: Barton ME, Peters SC, Shannon HE. Comparison of the effect of glutamate receptor modulators in the 6 Hz and maximal electroshock seizure models. Epilepsy Res. 2003 Sep;56(1):17-26. PubMed PMID: 14529950.

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