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MPEP

Cat. No. M2867
MPEP Structure
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50mg USD 220 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

MPEP is a selective antagonist for the metabotropic glutamate receptor subtype 5 (mGluR5) with IC50 of 36 nM. MPEP is a significantly more potent antagonist derived by structural derivatization around SIB-1757 and SIB-1893. MPEP has no agonist or antagonist activities at the human mGlu1b receptor expressed in CHO-K1 cells at concentrations up to 30 μM. When tested at group II and III receptors, MPEP does not show agonist or antagonist activity at 100 μM on human mGlu2, -3, -4a, -7b, and -8a receptors nor at 10 μM on the human mGlu6 receptor. MPEP has no significant effect at 100 μM on human NMDA (NMDA1A/2A), rat AMPA (Glu3-(flop)) and human kainate (Glu6-(IYQ)) receptor subtypes nor at 10 μM on the human NMDA1A/2B receptor. In rat neonatal brain slices, MPEP inhibits DHPG-stimulated PI hydrolysis with a potency and selectivity similar to that observed on human mGlu receptors. MPEP is centrally active following peripheral application and selectively inhibits group I agonist effects in the rat hippocampal CA1 area in vivo. MPEP produces anxiolytic-like effects in several tests such as the Vogel test in rats, the elevated plus-maze test in rats as well as the four-plate test in mice. MPEP also exerts antidepressant-like effects in the tail suspension test in mice. MPEP does not induce sedation nor disturb motor coordination in animals. [2] MPEP also acts as a positive allosteric modulator for the human metabotropic glutamate receptor 4 (hmGluR4). Blocking of mGluR5 with MPEP is able to rescue two major Fragile X Syndrome mouse model phenotypes. ?

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 193.24
Formula C14H11N
CAS Number 96206-92-7
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MPEP supplier, GluR, inhibitors

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