TCS 1102 MedChemExpress (MCE)

Product Name	N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
Synonyms	TCS-102 TCS 1102 N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide (2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide Synonyms TCS-102 TCS 1102 N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide (2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide (2S)- 2-Pyrrolidinecarboxamide, N-[1,1'-biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl] 2-PyrrolidinecarboxaMide, N-[1,1'-biphenyl]-2-yl-1-[2-[(1-Methyl-1H-benziMidazol-2-yl)thio]acetyl]-, (2S)- (2S)-N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl]-2-pyrrolidinecarboxamide TCS1102 TCS 1102 N-[1,1'-Biphenyl]-2-yl-1-[2-[(1-methyl-1H-benzimidazol-2-yl)thio]acetyl-2-pyrrolidinedicarboxamide
CAS	916141-36-1
EINECS
Chemical Formula	C27H26N4O2S
Molecular Weight	470.59
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Get quote
Descriptions	TCS 1102 TCS 1102 MedChemExpress (MCE) HY-10900 916141-36-1 99.73% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions TCS 1102 TCS 1102 MedChemExpress (MCE) HY-10900 916141-36-1 99.73% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. TCS 1102 is a potent, dual orexin receptor antagonist, with Ki values of 0.2 nM and 3 nM for OX2 and OX1 receptors, respectively. TCS 1102 demonstrates excellent blood-brain barrier penetrability and moderate bioavailability in rats. TCS 1102 (10 μM) inhibits Ca2+ responses to Orexin A (human, rat, mouse) (HY-106224) and Yan 7874 (an Orexin receptor agonist) in CHO-hOX2 cells[2]. TCS 1102 (compound 18) (15, 50, 100 mg/kg i.p single dose) induces locomotion inhibition in rat in a dose dependent manner[1]. TCS-1102 (10 and 20 mg/kg i.p. single dose) decreases fear and anxiety in rats after exposure to footshock. Furthermore, TCS-1102 (10 mg/kg i.p. single dose) also shows anxiolytic effects for high responders (HR) rat when tested in the elevated T-maze[3]. PK of TCS 1102 in Rat (100 mg/kg i.p. measured at 30 min)[1] CL (mL/min/kg) T1/2 (h) F (%) Brain/plasma/CSF (nM) 3.7 0.3 11 2370/3500/43 OX1 Receptor 3 nM (Ki) OX2 Receptor 0.2 nM (Ki) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [2]. Turku A, et al. Orexin receptor agonist Yan 7874 is a weak agonist of orexin/hypocretin receptors and shows orexin receptor-independent cytotoxicity. PLoS One. 2017 Jun 2 12(6):e0178526. [Content Brief] [3]. 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. [Content Brief]
Supplier Website	https://www.medchemexpress.com/TCS-1102.html
Last Update	2025-05-21 16:50:25

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