SB-334867 (Synonyms: SB 334867A) |
| Catalog No.GC13539 |
SB-334867(SB 334867A)은 탁월한 선택성 혈액뇌장벽 투과성 오렉신-1(OX1) 수용체 길항제로 OX2(pKb=7.4)보다 선택성을 나타내며 5-HT2B, 5-HT2C(pKi 포함)보다 100배 우수합니다. 각각 5.4와 5.3의 값.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 249889-64-3
Sample solution is provided at 25 µL, 10mM.
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SB-334867 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 can 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 is more selective for OX1 receptor over OX2 receptor. It causes 32.7% and 22% inhibition of orexin-A and orexin-B induced calcium responses in CHO-OX2 cells, respectively. Moreover, SB-334867 is found to reduce both orexin-A-induced and fasting-induced food intake. The acute anorectic effect of it is associated with signi®cant reductions in all active behaviours [1, 2].
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.
| Cell experiment [1]: | |
|
Cell lines |
CHO-OX1 and CHO-OX2 cells |
|
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. |
|
Reacting condition |
100 pM-10 μM |
|
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]: | |
|
Animal models |
adult male Lister hooded rats |
|
Dosage form |
3.0, 10.0 and 30.0 mg/kg, i.p. |
|
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. |
|
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. |
|
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. | |
| Cas No. | 249889-64-3 | SDF | |
| Synonyms | SB 334867A | ||
| Chemical Name | 1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea | ||
| Canonical SMILES | CC1=NC2=C(O1)C=C(C=C2)NC(=O)NC3=C4C(=NC=C3)C=CC=N4 | ||
| Formula | C17H14ClN5O2 | M.Wt | 355.78 |
| Solubility | ≥ 5.2mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8107 mL | 14.0536 mL | 28.1073 mL |
| 5 mM | 562.1 μL | 2.8107 mL | 5.6215 mL |
| 10 mM | 281.1 μL | 1.4054 mL | 2.8107 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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