FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.
Cat.No
DC9845
Name
FITM
Chemical Properties
CAS
932737-65-0
Formula
C18H18FN5OS
MW
371.4318
Storage
4°C for 1 year, -20°C for more than 2 years
References
[1]. Wu H, et al. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science. 2014 Apr 4;344(6179):58-64.
[2]. Bai Q, et al. Investigation of allosteric modulation mechanism of metabotropic glutamate receptor 1 by molecular dynamics simulations, free energy and weak interaction analysis. Sci Rep. 2016 Feb 18;6:21763.
[3]. Yamasaki T, et al. In vivo measurement of the affinity and density of metabotropic glutamate receptor subtype 1 in rat brain using 18F-FITM in small-animal PET. J Nucl Med. 2012 Oct;53(10):1601-7.
[4]. Xie L, et al. Molecular imaging of ectopic metabotropic glutamate 1 receptor in melanoma with a positron emission tomography radioprobe (18) F-FITM. Int J Cancer. 2014 Oct 15;135(8):1852-9.
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