A negative allosteric modulator of mGluR5
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RG-7090

Item No. 36806

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-chloro-4-[2-[1-(4-fluorophenyl)-2,5-dimethyl-1H -imidazol-4-yl]ethynyl]-pyridine
CAS Number
802906-73-6
Synonyms
  • Basimglurant
  • RO4917523
Molecular Formula
C18H13ClFN3
Formula Weight
325.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 0.5 mg/mlEthanol: Slightly soluble
λmax
236, 321 nm
SMILES
ClC1=CC(C#CC2=C(C)N(C3=CC=C(F)C=C3)C(C)=N2)=CC=N1
InChi Code
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
InChi Key
UPZWINBEAHDTLA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $94

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    5 mg

    $418

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    10 mg

    $742

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    25 mg

    $1,159

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    Product Description

    RG-7090 is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5).1 It binds to mGluR5 (Ki = 35.6 nM) and is selective for mGluR5 over a panel of 116 additional receptors at 10 µM. RG-7090 inhibits quisqualate-induced calcium mobilization and inositol phosphate accumulation in HEK293 cells expressing human mGluR5 (IC50s = 7 and 5.9 nM, respectively). In vivo, RG-7090 (10 and 30 mg/kg) reduces immobility time in the forced swim test in rats. It increases drinking time in the Vogel conflict drinking test and reduces stress-induced hyperthermia, indicating anxiolytic-like activity, in rats. RG-7090 (0.1-10 mg/kg, s.c.) inhibits surgical sciatic nerve constriction-induced cold allodynia in rats. It also increases the threshold of bladder filling volume to trigger the micturition reflex in anesthetized rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lindemann, L., Porter, R.H., Scharf, S.H., 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. 353(1), 213-233 (2015).