SB-334867 free base

SB-334867 free base

Catalog Number:
L002370520APE
Mfr. No.:
APE-B3423
Price:
$212
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          Background

          SB-334867 free base is a selective antagonist of orexin-1 receptor [1].
          Orexin-A and orexin-B are two peptides isolated from rat hypothalamus. They are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle.
          SB-334867 free base could inhibit the orexin-A and orexin-B induced calcium responses in CHO-OX1 cells with pKB values of 7.27 and 7.23, respectively. SB-334867 was more selective for OX1 receptor over OX2 receptor. It caused 32.7% and 22% inhibition of orexin-A and orexin-B induced calcium responses in CHO-OX2 cells, respectively. Moreover, SB-334867 was found to reduce both orexin-A-induced and fasting-induced food intake. The acute anorectic effect of it was associated with significant reductions in all active behaviours [1, 2].

          [1] Smart D, Sabido-David C, Brough S J, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. British journal of pharmacology, 2001, 132(6): 1179-1182.
          [2] Rodgers R J, Halford J C G, Nunes de Souza R L, et al. SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. European Journal of Neuroscience, 2001, 13(7): 1444-1452.

      • Properties
        • Categories
          orexin-1 receptor antagonist, selective
          Alternative Name
          1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
          CAS Number
          792173-99-0
          Molecular Formula
          C17H13N5O2
          Molecular Weight
          319.32
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥14.55 mg/mL in DMSO
          Storage
          Store at -20°C
          SMILES
          CC1=NC2=C(O1)C=C(C=C2)NC(=O)NC3=C4C(=NC=C3)C=CC=N4

          * For Research Use Only

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