CTEP Derivative


Catalog No. size PriceQuantity
M6406-2 2mg solid $80
M6406-10 10mg solid $320

Description

Cas:802906-73-6

Product Information

CTEP Derivative is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.

 

IC50 & TargetmGlu5 Receptor

 

  • nM (Kd)

 

Molecular Weight:325.77

 

Formula:C₁₈H₁₃ClFN₃

 

Smiles Code:

CC1=C(C#CC2=CC(Cl)=NC=C2)N=C(C)N1C3=CC=C(F)C=C3

 

Shipping:

Room temperature in continental US; may vary elsewhere.

 

Storage:

Powder     -20°C    3 years

4°C    2 years

In solvent -80°C    6 months

-20°C 1 month

 

In Vitro:

[3H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with Kd of 1.1 nM. In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation with an IC50 of 5.9 nM. Basimglurant (RG7090) shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues.

 

In Vivo:

Basimglurant (RG7090) is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg).

 

 

References

 

  1. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33.

 

  1. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.

 

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

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed