CTEP Derivative
CTEP Derivative Basic information
- Product Name:
- CTEP Derivative
- Synonyms:
-
- CTEP Derivative
- BasiMglurant
- RG 7090
- RG7090
- RG-7090
- 2-Chloro-4-((1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-yl)ethynyl)pyridine
- RG7090(Basimglurant)
- 2-Chloro-4-[2-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-yl]ethynyl]pyridine
- CAS:
- 802906-73-6
- MF:
- C18H13ClFN3
- MW:
- 325.77
- Mol File:
- 802906-73-6.mol
CTEP Derivative Chemical Properties
- Melting point:
- 132 - 135°C
- Boiling point:
- 526.6±60.0 °C(Predicted)
- Density
- 1.21±0.1 g/cm3(Predicted)
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 5.27±0.70(Predicted)
- form
- Solid
- color
- Pale Brown to Light Brown
- Stability:
- Hygroscopic, Moisture Sensitive
- InChI
- InChI=1S/C18H13ClFN3/c1-12-17(8-3-14-9-10-21-18(19)11-14)22-13(2)23(12)16-6-4-15(20)5-7-16/h4-7,9-11H,1-2H3
- InChIKey
- UPZWINBEAHDTLA-UHFFFAOYSA-N
- SMILES
- C1(Cl)=NC=CC(C#CC2=C(C)N(C3=CC=C(F)C=C3)C(C)=N2)=C1
CTEP Derivative Usage And Synthesis
Uses
Basimglurant is a potent, selective and orally available mGlu5 negative allosteric modulator for the treatment of mood disorders.
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[1]. 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)[2].
IC 50
mGlu5 Receptor: 1.1 nM (Kd)
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