1. Neuronal Signaling
  2. Amyloid-β
  3. 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine

4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine 

Cat. No.: HY-111513 Purity: 98.60%
Handling Instructions

4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM.

For research use only. We do not sell to patients.

4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine Chemical Structure

4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine Chemical Structure

CAS No. : 566169-98-0

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Description

4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM.

IC50 & Target

Ki: 1.7 nM (Amyloid-β)[1]

In Vivo

Alzhermer's Disease (AD) is a neurodegenerative illness characterized by memory loss and other cognitive deficits. The ability to quantify amyloid load before treatment is critical to the efficient development of this class of drugs[2]. Brain entry in control mice and baboons is high for 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine. Staining of AD frontal cortex tissue sections with 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine indicates the selective binding of the compound to amyloid plaques and cerebrovascular amyloid. The encouraging properties of the compound support the choice of this derivative for further evaluation in human subject studies of brain Amyloid-βdeposition. The brain radioactivity concentrations (%ID-kg/g) of 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is remarkably similar in mice and baboons (0.21 vs 0.27). The rate of clearance of radioactivity is considerably slower from baboon brain than from mouse brain, although the rank order of clearance rate is similar in mice and baboons. The tissue staining findings utilizing nonradiolabeled, fluorescent 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine are similar to those reported for BTA-1. Both amyloid plaques and cerebrovascular amyloid are stained by 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine in a manner similar to serial sections stained with an antibody to Amyloid-β, and relatively little tissue background staining is observed[1].

Molecular Weight

319.22

Formula

C₁₄H₁₁BrN₂S

CAS No.

566169-98-0

SMILES

CNC1=CC=C(C2=NC3=CC=C(Br)C=C3S2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

References
Animal Administration
[1]

Mice[1]

Studies are performed in female Swiss-Webster mice (23-35 g). The mice are injected in a lateral tail vein with 0.37-3.7 MBq (10-100 µCi) of a high specific activity (>7.4 GBq/µmol) 11C-4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine contained in <0.10 mL of a solution of 93% isotonic saline and 7% ethanol. The mice are anesthetized and killed by cardiac excision following cardiac puncture to obtain arterial blood samples at 2 or 30 min postinjection. The mouse brains are rapidly excised and divided into cerebellum and remaining whole brain (including brain stem) fractions. The brain samples are counted in a gamma wellcounter, and the counts are decay-corrected to the time of injection relative to 11C standards prepared from the injection solution to determine the percent injected dose (%ID) in the samples. The brain samples are weighed to determine the percent injected dose per gram tissue (%ID/g), and this quantity is multiplied by the whole body weight (in kg) to determine the body-weight normalized radioactivity concentration [(%ID-kg)/g] of each tissue sample[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine
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HY-111513
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