Language:English
Language:

Xcessbio

Place your promotion here

You have no items in your shopping cart.

CTEP, mGlu5 Antagonist

CTEP, mGlu5 Antagonist

$259.00
A highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor.
Catalog No. Unit Price Qty
M60099-5s 5 mg solid $259.00
M60099-25s 25 mg solid $690.00

Details

Product Information
Molecular Weight: 391.77
Formula: C19H13ClF3N3O
Purity: ≥ 98%
CAS#: 871362-31-1
Solubility: DMSO up to 100 mM
Chemical Name: 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Details

 

Biological Activity:

CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM. It shows >1000-fold selectivity against 103 targets, including all known mGlu receptors. CTEP can penetrate the brain with a brain/plasma ratio of 2.6.  CTEP is active in the stress-induced hyperthermia procedure in mice and the Vogel conflict drinking test in rats with minimal effective doses of 0.1 and 0.3 mg/kg, respectively, reflecting a 30- to 100-fold higher in vivo potency compared with 2-methyl-6-(phenylethynyl)pyridine (MPEP) and fenobam. CTEP is the first reported mGlu5 inhibitor with both long half-life of approximately 18 h and high oral bioavailability allowing chronic treatment with continuous receptor blockade with one dose every 48 h in adult and newborn animals. Acute CTEP treatment corrects elevated hippocampal long-term depression, protein synthesis, and audiogenic seizures. Chronic treatment that inhibits mGlu5 within a receptor occupancy range of 81% ± 4% rescues cognitive deficits, auditory hypersensitivity, aberrant dendritic spine density, overactive ERK and mTOR signaling, and partially corrects macroorchidism. By enabling long-term treatment through a wide age range, CTEP allows the exploration of the full therapeutic potential of mGlu5 inhibitors for indications requiring chronic receptor inhibition.

 

How to Use:

  • In vitro:  CTEP was used at 0.03-0.1 µM final concentration in vitro and in cellular assays.
  • In vivo: CTEP was orally dosed to mice at single 0.1-1.0 mg/kg, or with a dose of 2 mg/kg orally every 48 h for 2 months.  CTEP was orally dose at 2 mg/kg BID achieves uninterrupted mGlu5 occupancy per 48 hours in mice.

 

Reference:

  • 1. Lindemann L, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. (2011) J Pharmacol Exp Ther. 339(2):474-86.
  • 2. Michalon A, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. (2012) Neuron. 74(1):49-56.







Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 391.77
Formula: C19H13ClF3N3O
Purity: ≥ 98%
CAS#: 871362-31-1
Solubility: DMSO up to 100 mM
Chemical Name: 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Details

 

Biological Activity:

CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM. It shows >1000-fold selectivity against 103 targets, including all known mGlu receptors. CTEP can penetrate the brain with a brain/plasma ratio of 2.6.  CTEP is active in the stress-induced hyperthermia procedure in mice and the Vogel conflict drinking test in rats with minimal effective doses of 0.1 and 0.3 mg/kg, respectively, reflecting a 30- to 100-fold higher in vivo potency compared with 2-methyl-6-(phenylethynyl)pyridine (MPEP) and fenobam. CTEP is the first reported mGlu5 inhibitor with both long half-life of approximately 18 h and high oral bioavailability allowing chronic treatment with continuous receptor blockade with one dose every 48 h in adult and newborn animals. Acute CTEP treatment corrects elevated hippocampal long-term depression, protein synthesis, and audiogenic seizures. Chronic treatment that inhibits mGlu5 within a receptor occupancy range of 81% ± 4% rescues cognitive deficits, auditory hypersensitivity, aberrant dendritic spine density, overactive ERK and mTOR signaling, and partially corrects macroorchidism. By enabling long-term treatment through a wide age range, CTEP allows the exploration of the full therapeutic potential of mGlu5 inhibitors for indications requiring chronic receptor inhibition.

 

How to Use:

  • In vitro:  CTEP was used at 0.03-0.1 µM final concentration in vitro and in cellular assays.
  • In vivo: CTEP was orally dosed to mice at single 0.1-1.0 mg/kg, or with a dose of 2 mg/kg orally every 48 h for 2 months.  CTEP was orally dose at 2 mg/kg BID achieves uninterrupted mGlu5 occupancy per 48 hours in mice.

 

Reference:

  • 1. Lindemann L, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. (2011) J Pharmacol Exp Ther. 339(2):474-86.
  • 2. Michalon A, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. (2012) Neuron. 74(1):49-56.







Products are for research use only. Not for human use.

Reviews

Write Your Review

How do you rate this product? *

Price:
Value:
Quality: