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Tocris/LY 341495/1209/1/1 mg

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货号: 1209/1

品牌: Tocris

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Description: Highly potent, selective group II antagonist

Chemical Name: (2S)-2-Amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Highly potent and selective group II metabotropic glutamate receptor antagonist (K_i/IC₅₀ values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu₂, mGlu₃, mGlu₈, mGlu_7a, mGlu_1a, mGlu_5a and mGlu_4a receptors respectively). Readily brain penetrant and active in vivo. Disodium salt (Cat. No. 4062) also available. Also available as part of the Group II mGlu Receptor Tocriset™, Group III mGlu Receptor Tocriset™ and Mixed mGlu Receptor Tocriset™.

Licensing Information

Sold with the permission of Eli Lilly and Company

Technical Data

M. Wt	353.37
Formula	C₂₀H₁₉NO₅
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	201943-63-7
PubChem ID	9819927
InChI Key	VLZBRVJVCCNPRJ-KPHUOKFYSA-N
Smiles	[H][C@]4([C@@H]([C@](O)=O)C4)[C@](N)(C(O)=O)CC2C3=C(C=CC=C3)OC1=CC=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	1.2eq. NaOH	35.34	100
	DMSO	3.61	10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 353.37. Batch specific molecular weights may vary from batch to batch due to solvent 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	2.83 mL	14.15 mL	28.3 mL
5 mM	0.57 mL	2.83 mL	5.66 mL
10 mM	0.28 mL	1.41 mL	2.83 mL
50 mM	0.06 mL	0.28 mL	0.57 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Fitzjohn et al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology 37 1445 PMID: 9886667

Johnson et al (1999) [³H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology 38 1519 PMID: 10530814

Kingston et al (1998) LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology 37 1 PMID: 9680254

Ornstein et al (1998) 2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl) glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioav J.Med.Chem. 41 358 PMID: 9464367

Keywords: LY 341495, supplier, Group, II/III, antagonists, potent, selective, group, II, mGlur, III, Receptors, mGlu4, mGlu6, mGlu7, mGlu8, mGlu4R, mGlu6R, mGlu7R, mGlu8R, Glutamate, Metabotropic, mGlu2, mGlu3, mGluR2, mGluR3, LY341495, Glutamate, (Metabotropic), Group, II, Receptors, Glutamate, (Metabotropic), Group, III, Receptors, Glutamate, (Metabotropic), Group, II, Receptors, Tocris Bioscience

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