The formation of β-amyloid (Aβ) plaques is a key neurodegenerative event in Alzheimer's disease (AD). Since the imaging of these plaques in vivo may
lead to the presymptomatic diagnosis of AD, many molecular probes for this purpose including PET/SPECT and MRI tracers, have been developed. The PET ligand [11C]
-2-(4-(methylamino) phenyl)-6-hydroxybenzothiazole (PIB) with a benzothiazole backbone has shown particular promise in early clinical trials and is currently being used in
a number of human studies.
PP-BTA-1 is a newly developed push-pull benzothiazole derivative as a fluorescent probe for detecting β-amyloid plaques in Alzheimer's brains.
It consists of benzothiazole as the highly polarized bridge, a dimethylamino group as the donor, and a dicyanomethylene group as the acceptor.
- Easy detection by a fluorescence detector in Alzheimer's brains
- No conventional device or instrument such as RI or PET for clinical research
- Less adverse effects on absorption by self-fluorescence or biogenic factors in histological staining because of the wavelength of PP-BTA-1 is close to the
- Selective binding to β-Amyloid protein
- Stronger binding to Aβ than that of PIB
Leaflet (377 KB/2p)
C13H10N4S = 254.31
Solubility: Soluble in ethanol
Ex/Em = 540/634 nm (in EtOH)
Application < Histological Section Staining >
Fig. 1 Investigation in an animal model of AD, the TG2576 mouse
Neuropathological staining of PP-BTA-1 in 10μm brain section from an animal model of AD, the Tg2576 mouse (A) and a wild-type normal mouse (C). Aβ plaques
labeled with PP-BTA-1 were confirmed by staining of the serial section using thioflavin S (B).
Senile plaques on Tg2576 mouse brain section were selectively fluorescent-stained with PP-BTA-1 (A) as well as thioflavin S (B).
On the other hand, no parts on wild-type normal mouse brain sections were stained with PP-BTA-1 (C).
Fig. 2 Investigation in human AD brain sections|
Neuropathological staining of 5 μm AD brain sections from the temporal cortex (A, B) and adult normal temporal brain section(C). Many neuritic plaques are clearly
stained with PP-BTA-1(A). Intense fluorescence can be seen in the core of neuritic plaques. Aβ immunostaining with anti Aβantibodies in the serial sections
shows an identical staining pattern of plaques(B).
Senile plaques on AD brain section were selectively fluorescent-stained with PP-BTA-1 (A) as well as anti Aβ antibody. On the other hand, no parts on an adult
normal temporal brain section (C).
(Data was provided by Masahiro Ono and Hideo Saji at School of Pharmaceutical Sciences, Kyoto University)
- Ono, M. et al.: "Push-pull benzothiazole derivatives as probes for detecting β-amyloid plaques in Alzheimer's brains", Bioorg. Med. Chem.,
17, 7002-7 (2009).
- Ono, M.: "Development of Positron-Emission Tomography/Single-Photon Emission Computed
Tomography Imaging Probes for in Vivo Detection of β-Amyloid Plaques in Alzheimer's Brains", Chem. Pharm. Bull., 57(10), 1029-39
||Wako Catalog No. (Package Size)
< for Cellbiology >
|165-25301 (1 mg)
||2 ~ 10 °C
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