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Basimglurant

Catalog No. T12717Cas No. 802906-73-6
Alias RG7090, CTEP Derivative

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

Basimglurant

Basimglurant

Purity: 99.38%
Catalog No. T12717Alias RG7090, CTEP DerivativeCas No. 802906-73-6
Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM).
Pack SizePriceAvailabilityQuantity
1 mg$76In Stock
5 mg$178In Stock
10 mg$266In Stock
25 mg$439In Stock
50 mg$592In Stock
100 mg$738In Stock
200 mg$998In Stock
1 mL x 10 mM (in DMSO)$205In Stock
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Purity:99.38%
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Product Introduction

Bioactivity
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].
AliasRG7090, CTEP Derivative
Chemical Properties
Molecular Weight325.77
FormulaC18H13ClFN3
Cas No.802906-73-6
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM3.0697 mL15.3483 mL30.6965 mL153.4825 mL
5 mM0.6139 mL3.0697 mL6.1393 mL30.6965 mL
10 mM0.3070 mL1.5348 mL3.0697 mL15.3483 mL
20 mM0.1535 mL0.7674 mL1.5348 mL7.6741 mL
50 mM0.0614 mL0.3070 mL0.6139 mL3.0697 mL
100 mM0.0307 mL0.1535 mL0.3070 mL1.5348 mL

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