产品概述
A collection of 6 antagonists for mGlu receptor subtypes. Products are freeze-dried to an exact weight so that addition of 1 ml or 0.5 ml of solvent provides a stock solution of 5 mM or 10 mM, respectively. The kit contains LY 341495 sodium salt (ab120400), (R,S)-MCPG sodium salt (ab120252), LY 367385 sodium salt (ab120418), YM 298198 hydrochloride (ab120015), MTEP hydrochloride (ab120035) and MMPIP (ab120245).
Receptor
Description
All mGlu
(mGlu1,2,3,4,5,6,7,8)
LY 341495 sodium salt:
Very selective nanomolar potent antagonist for group II mGlu receptors. Also a relatively potent antagonist for group III mGlu receptors at high nanomolar to low micromolar concentrations. Kd values are 1.67, 0.75, 31.6, 72.7, 14 nM at human mGlu2, mGlu3, mGlu6, mGlu7a, and human mGlu8a receptors, respectively. IC50 values are 7.8, 8.2 and 22 M for mGlu1a, mGlu5a and mGlu4 receptors, respectively. Readily brain penetrant and active in vivo.
Suggested Solvent: Water
Goup I II
(R,S)-MCPG sodium salt:
Group I / group II metabotropic glutamate receptor antagonist. Water soluble form.
Suggested Solvent: Water
mGlu1
LY 367385 sodium salt:
Potent, selective mGlu1a antagonist. Neuroprotective and anticonvulsant in vivo.
Suggested Solvent: Water
mGlu1
YM298198 hydrochloride:
Potent, selective, water-soluble, non-competitive mGlu1 antagonist (IC50 = 16 nM) Selective over mGlu2,3,4,5,6 and 7 and ionotropic receptors (IC50 10 M). Orally active analgesic in vivo.
Suggested Solvent: Water
mGlu5
MTEP hydrochloride:
Brain penetrant, potent, selective and non-competitive mGlu5 receptor antagonist (IC50 = 5 nM in Ca2+-flux assay; Ki = 16 nM). In vivo anxiolytic, devoid of side effects seen with MPEP and benzodiazepines.
Suggested Solvent: Water
mGlu7
MMPIP:
Potent, selective allosteric antagonist at mGlu7 receptors. Inhibits agonist-induced intracellular calcium mobilisation and cAMP accumulation (IC50 values are 26 and 610 nM). Also displays intrinsic activity; increasing forskolin-induced cAMP accumulation in the absence of an agonist. Exhibits no significant activity at mGluR1, mGluR2, mGluR3, mGluR4, mGluR5, and mGluR8.
Suggested Solvent: DMSO
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 6 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20 C. Generally, these will be useable for up to one week. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
KIT
Metabotropic Glutamate Receptor contains a Periplasmic Binding Protein Type 1 region, which belongs to Type 1 periplasmic binding fold superfamily. This model and hierarchy represent the ligand binding domains of the LacI family of transcriptional regulators, periplasmic binding proteins of the ABC-type transport systems.
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
Click here to view the general protocols
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