A positive allosteric modulator of mGluR7 and mGluR8
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VU6005649

Item No. 43138

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(2,3-difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)-pyrazolo[1,5-a]pyrimidine
CAS Number
2137047-43-7
Molecular Formula
C16H12F5N3O
Formula Weight
357.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
FC1=C(C(C2=C3N=C(C)C=C(C(F)(F)F)N3N=C2C)=CC=C1OC)F
InChi Code
InChI=1S/C16H12F5N3O/c1-7-6-11(16(19,20)21)24-15(22-7)12(8(2)23-24)9-4-5-10(25-3)14(18)13(9)17/h4-6H,1-3H3
InChi Key
NYBZCKAQIIPSDS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $76

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    10 mg

    $121

    Add

    25 mg

    $228

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    50 mg

    $380

    Add
    Product Description

    VU6005649 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 7 (mGluR7) and mGluR8.1 It enhances calcium mobilization induced by L-AP4 (Item No. 14538) in HEK cells expressing mGluR7 or mGluR8 (EC50s = 0.65 and 2.6 µM, respectively). It is selective for mGluR7 and mGluR8 over mGluR1-6, as well as a panel of 67 GPCRs, ion channels, transports, and nuclear hormone receptors, at 10 µM but does inhibit the neurokinin-1 (NK1) receptor (IC50 = 3.4 µM). In vivo, VU6005649 (50 mg/kg, i.p) increases the length of freezing time induced by contextual fear conditioning in mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Abe, M., Seto, M., Gogliotti, R.G., et al. Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5- a]pyrimidines. ACS Med. Chem. Lett. 8(10), 1110-1115 (2017).