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Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $76 | In Stock | |
5 mg | $178 | In Stock | |
10 mg | $266 | In Stock | |
25 mg | $439 | In Stock | |
50 mg | $592 | In Stock | |
100 mg | $738 | In Stock | |
200 mg | $998 | In Stock | |
1 mL x 10 mM (in DMSO) | $205 | In Stock |
Description | Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). |
Targets&IC50 | mGlu5 receptor:1.1 nM (Kd) |
In vitro | 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 (IC50 of 5.9 nM). Basimglurant shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues[1]. |
In vivo | Basimglurant is selective and safe inhibitor of mGlu5 with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. Basimglurant has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features[1]. |
Alias | RG7090, CTEP Derivative |
Molecular Weight | 325.77 |
Formula | C18H13ClFN3 |
Cas No. | 802906-73-6 |
Smiles | Cc1nc(C#Cc2ccnc(Cl)c2)c(C)n1-c1ccc(F)cc1 |
Relative Density. | 1.21 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (184.18 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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