|1-(2-甲基苯并[d]恶唑-6-基)-3-(1,5-萘啶-4-基)脲|CsnPharm

CAS No.: 792173-99-0

1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea Catalog No. CSN11489

Synonyms: SB334867A free base;SB-334867

SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with pKb of 7.2.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 OX Receptor 1

pKb:7.2
描述SB-334867-A is the first selective and non-peptide orexin-1 receptor antagonist with pK_B 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.
动物研究
剂量
Rat: 0.01 mg/kg - 10 mg/kg^[4] (i.p.), 30 mg/kg^[5] (i.p.); 2 mg/kg^[6] (i.v.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Rat: 0.01 mg/kg - 10 mg/kg^[4] (i.p.), 30 mg/kg^[5] (i.p.); 2 mg/kg^[6] (i.v.)
给药途径	i.p., i.v.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1317 mL
- 15.6584 mL
- 31.3168 mL
- 5 mM
- 0.6263 mL
- 3.1317 mL
- 6.2634 mL
- 10 mM
- 0.3132 mL
- 1.5658 mL
- 3.1317 mL

技术信息

CAS号

792173-99-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H13N5O2

运输

蓝冰

分子量

319.32

别名

SB334867A free base;SB-334867

溶解度

DMSO	120.0 mg/mL (375.8 mM) warming
Water	insoluble

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

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1-(2-Methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea Catalog No. CSN11489

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