mGlu Antagonists试剂盒

概述

• 产品名称
  mGlu Antagonists试剂盒
  参阅全部 Metabotropic glutamate receptor 试剂盒
• 特异性
  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).
• 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
  (mGlu_{1,2,3,4,5,6,7,8}) 

  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. K_d values are 1.67, 0.75, 31.6, 72.7, 14 nM at human mGlu₂, mGlu₃, mGlu₆, mGlu_7a, and human mGlu_8a receptors, respectively. IC₅₀ values are 7.8, 8.2 and 22 µM for mGlu_1a, mGlu_5a 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 mGlu_1a 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 mGlu_2,3,4,5,6 and ₇ and ionotropic receptors (IC₅₀ > 10 µM). 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; K_i = 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 (IC₅₀values 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 

• 说明

  KIT

性能

• 存放说明
  Store at -20°C. Please refer to protocols.