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SB-334867 HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB-334867 HCl图片
CAS NO:249889-64-3
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)319.32
FormulaC17H14NClN5O2
CAS No.249889-64-3 (HCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 63 mg/mL (197.3 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (9.4 mM)
Solubility (In vivo)1% CMC Na: 30 mg/mL
SynonymsSB334867A; SB334867; SB 334867; SB334867 HCl; SB334867 hydrochloride; SB-334867A; SB 334867A;
实验参考方法
In Vitro

In vitro activity: In CHO-OX1 cells, SB-334867 inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses with pKB of 7.27 and 7.23 respectively, without effect on the UTP (3 microM)-induced calcium response.


Kinase Assay: SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. IC50 value: 7.2 (pKb). SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A).


Cell Assay: 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.

In VivoIn both male and female rats, SB-334867 (30 mg/kg, i.p.) significantly reduces natural and orexin-A-induced food intake. SB-334867 (2 mg/kg, i.v.) blocks the effects of antipsychotic drugs on dopamine neuronal activity in rats. SB-334867 also inhibits the development of morphine analgesic tolerance in rats.
Animal modelMale and female Sprague–Dawley rats
Formulation & DosageDissolved in 10% (w/v) Encapsin in sterile water; 30 mg/kg; i.p. administration
ReferencesBr J Pharmacol. 2001 Mar;132(6):1179-82; Regul Pept. 2000 Dec 22;96(1-2):45-51; Neuropsychopharmacology. 2007 Apr;32(4):786-92.