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Product name : TCS 1102
Item : CR1785
Price : 100mg, $745; 200mg, $1185
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CAS : 916141-36-1
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Details:
 Chemical Information
M.Wt 470.59 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C27H26N4O2S
CAS No 916141-36-1
Solubility

100 mM in DMSO; 100 mM in ethanol



Biological Activity of TCS 1102

 

TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
IC50 value: 0.2 nM (Ki, OX2 receptor); 3 nM (Ki, OX1 receptor) [1]
Target: OX2 and OX1 receptor
TCS-1102 (10 and 20 mg/kg, i.p.) were found to decrease fear and anxiety in rats 14 days after exposure to footshock.Furthermore, TCS-1102 (10 mg/kg, i.p.) was found to have anxiolytic effects that were specific for HR when tested in the elevated T-maze. [2]

 

[1]. Bergman JM, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1425-30.
[2]. Chen X, et al. Orexins (hypocretins) contribute to fear and avoidance in rats exposed to a single episode of footshocks. Brain Struct Funct. 2013 Aug 18.


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