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SB-334867 free base

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Chemical Structure| 792173-99-0 同义名 : SB334867A free base;SB-334867
CAS号 : 792173-99-0
货号 : A284699
分子式 : C17H13N5O2
纯度 : 99%+
分子量 : 319.317
MDL号 : MFCD06411602
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(156.58 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

0.1 M HCL: 5 mg/mL(15.66 mM)，配合低频超声，并调节pH至3
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 2.4 mg/mL clear

PO 0.5% CMC-Na 80 mg/mL suspension

生物活性
靶点

  • OX1 receptor
描述 SB-334867-A is the first selective and non-peptide orexin-1 receptor antagonist with pKB values of 7.27 and 7.23 for inhibition of the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses, respectively, but had no effect on the UTP (3μM)-induced calcium response in CHO-OX1 cells. SB-334867-A inhibited OX2 mediated calcium responses up to 10μM. A single intraperitoneal injection with SB-334867-A at dose of 30mg/kg during the light phase reduced both orexin-A-induced food intake and feeding stimulated by an overnight fast for 4h in male rats. Daily injections with SB-334867-A at the start of the dark phase for 3 days reduced natural feeding in male rats over 24 h on day 1 and day 3. SB-334867-A possesses blood–brain barrier permeability shown as CNS penetration ratio brain/blood ratio of 0.4:1.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.66mL

3.13mL

1.57mL

31.32mL

6.26mL

3.13mL
参考文献

[1]Smart D, Sabido-David C, et al. SB-334867-A: the first selective orexin-1 receptor antagonist. Br J Pharmacol. 2001 Mar;132(6):1179-82.

[2]Haynes AC, Jackson B, et al. A selective orexin-1 receptor antagonist reduces food consumption in male and female rats. Regul Pept. 2000 Dec 22;96(1-2):45-51.

[3]Porter RA, Chan WN, et al. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10.