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TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1. TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor.
| Molecular Weight | 397.51 |
| Formula | C23H31N3O3 |
| CAS Number | 372523-75-6 |
| Solubility (25°C) | DMSO 20 mg/mL Ethanol 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related OX Receptor Products |
|---|
| MK-6096
MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R. |
| Almorexant
Almorexant is a competitive OX1 and OX2 orexin receptor antagonist with IC50 of 13 and 8 nM, respectively. |
| SB408124
SB408124 (Tocris-1963) is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
| MK-3697
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM. |
| 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). |
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Products are for research use only. Not for human use. We do not sell to patients.
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