SB-334867 hydrochloride
SB-334867 hydrochloride (CAS 249889-64-3) is a selective antagonist of the orexin-1 (OX1) receptor, a receptor implicated in several physiological roles including feeding behavior, energy balance, and sleep-wake regulation. In vitro studies using CHO cells expressing human OX1 receptor showed that SB-334867 inhibits orexin-A and orexin-B induced calcium mobilization (pKB values of 7.27 and 7.23, respectively), with limited activity at the orexin-2 (OX2) receptor subtype. In animal models, SB-334867 has been shown to reduce orexin-A-stimulated feeding as well as fasting-induced food intake, thus serving as a useful pharmacological tool in obesity, appetite regulation, and energy metabolism research.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 355.78 |
| Cas No. | 249889-64-3 |
| Formula | C17H14ClN5O2 |
| Solubility | insoluble in H2O; ≥2.72 mg/mL in EtOH with ultrasonic; ≥5.2 mg/mL in DMSO with gentle warming |
| Chemical Name | 1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | O=C(NC1=CC=NC2=CC=CN=C12)NC3=CC=C4N=C(C)OC4=C3.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
CHO-OX1 and CHO-OX2 cells |
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Preparation method |
The solubility of this compound in DMSO is >5.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
100 pM-10 μM |
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Applications |
In CHO-OX1 cells, SB-334867-A (100 pM-10 μM) inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses in a concentration-dependent way, with apparent pKB values of 7.27±0.04 and 7.23±0.03, respectively. In CHO-OX2 cells, SB-334867-A also inhibited the orexin-A (10 nM) and orexin-B (10 nM)-induced calcium responses by 32.7±1.9 and 22.0±4.0%, respectively. |
| Animal experiment [2]: | |
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Animal models |
adult male Lister hooded rats |
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Dosage form |
3.0, 10.0 and 30.0 mg/kg, i.p. |
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Application |
In adult male Lister hooded rats, SB-334867 significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. SB-334867 dose-dependently blocked the effects of orexin-A, such as stimulation of food intake, increasing grooming and delaying the onset of behavioural satiety. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [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. |
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Quality Control & MSDS
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Chemical structure
