Almorexant HCl

For research use only. Not for use in humans.

目录号:S2160 别名: ACT-078573 HCl 中文名称:阿莫伦特盐酸盐

Almorexant HCl Chemical Structure

CAS No. 913358-93-7

Almorexant HCl (ACT-078573)是口服有效的双重orexin receptor 拮抗剂,其作用于受体 OX1 和 OX2 的 IC50 分别为 6.6 nM 和 3.4 nM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2530.71 现货
RMB 1378.88 现货
RMB 2621.66 现货
RMB 7938.74 现货
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客户使用Selleck生产的Almorexant HCl发表文献3篇:

客户使用该产品的1个实验数据:

  • (C) No significant changes were observed compared with PBS control (n = 5) when sSNA is measured as % range. Grouped data for the % range from every treatment group are compared. AXT at 75 mg/kg (n = 4) produced no effect on baseline sympathetic activity. (D) AXT at 30 mg/kg (n = 5) and 75 mg/kg (n = 5) attenuated the effect of intermittent orexin-A (10 pmol×10; n = 5) on sSNA. Statistical significance was determined using one-way analysis of variance followed by Holm-Sidak correction to compare the effects with the control. Data are expressed as mean±S.E.M. ****P<0.0001; ***P<0.001; *P <0.05. #P<0.05 compared with intermittent orexin-A (10 pmol×10).

    J Pharmacol Exp Ther, 2016, 358(3):492-501. . Almorexant HCl purchased from Selleck.

产品安全说明书

OX Receptor抑制剂选择性比较

生物活性

产品描述 Almorexant HCl (ACT-078573)是口服有效的双重orexin receptor 拮抗剂,其作用于受体 OX1 和 OX2 的 IC50 分别为 6.6 nM 和 3.4 nM。
特性 口服生物可利用的食欲肽受体拮抗剂处于III期临床试验,用于治疗失眠症。
靶点
OX2 receptor [1] OX1 receptor [1]
3.4 nM 6.6 nM
体外研究

Almorexant抑制10 nM人食欲肽-A诱导的细胞内Ca2+的增加,在中国仓鼠卵巢细胞中,对OX1受体的IC50为16 nM (大鼠) 和13 nM (人),对OX2受体的IC50为15 nM (大鼠) 和8 nM (人)。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO NFjFfotHfW6ldHnvckBie3OjeR?= MkfqN|AhdWmwcx?= MmrWSIl{eGyjY3Xt[Y51KG:oIGuxNlVKZS2RcnX4bY4hSSCocn;tJIh2dWGwIF;YNnIh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDh[pRmeiB|MDDtbY5{KGK7IITvdINwfW62IHHuZYx6e2m|LDDLbUA:KDBwMEC0O{DPxE1w NH\2UmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK2O|AxPCd-MkWyOlcxODR:L3G+
CHO NYP3V3h{TnWwY4Tpc44h[XO|YYm= MXnBcpRi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJG9ZOlJiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJI9z\Xirbj3BMYlv\HWlZXSgbY51emGlZXzseYxieiClYXzjbZVuKHKnbHXhd4UtKEmFNUCgQUAxNjByODFOwG0v NFvu[lA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOxO|U6OSd-Mk[zNVc2QTF:L3G+
CHO MYHGeY5kfGmxbjDhd5NigQ>? MmrORY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBQYDKUIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk[WylaYXtJI1w[mmuaYrheIlwdiCkeTDGUGlRWiCjc4PhfUwhUUN3MDC9JFAvODB6IN88UU4> NIjnV|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{exPVI{OSd-MkO3NVkzOzF:L3G+
CHO Mmj6SpVv[3Srb36gZZN{[Xl? NYP2UIlTSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCRWEHSJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCxcnX4bY4uSS2rbnT1Z4VlKGmwdILhZ4VtdHWuYYKgZ4Ft[2m3bTDy[Yxm[XOnLDDJR|UxKD1iMD6wNVMh|ryPLh?= Ml3xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|MUe1PVEoRjJ4M{G3OVkyRC:jPh?=
CHO M3vvVGZ2dmO2aX;uJIF{e2G7 MmLTRY51[WexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBQYDGUIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk[WylaYXtJI1w[mmuaYrheIlwdiCkeTDGUGlRWiCjc4PhfUwhUUN3MDC9JFAvODF|IN88UU4> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdzOUKzNUc,OjN5MUmyN|E9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PhosphoTyr / SHP2; 

PubMed: 29467942     


Orexin-A and almorexant promote tyrosine phosphorylation of SHP2/OX1R complex. AsPC-1 cells preincubated or not with the SHP2 inhibitor NSC-87877 (50 μM) were challenged for 5 min without or with 1 μM orexin-A or 1 μM almorexant. In parallel, HPAF-II cells were also challenged for 5 min without or with 1 μM orexin-A. After cell lysis, anti-SHP2 antibodies were used to obtain anti-SHP2 immunoprecipitates (IP) from 500 μg of lysate protein. Western blot analysis was then performed using the antibodies anti-PhosphoTyrosine and anti-SHP2.

29467942
Growth inhibition assay
Tumor volume; 

PubMed: 29467942     


Effect of daily inoculation of almorexant on the growth of tumors developed by xenografting human PDCA cells in nude mice - (A) AsPC-1 cells were inoculated in the flank of nude mice at day 0. Mice were injected daily intraperitoneally with 100 μl of almorexant (1.8 μmol/kg) solutions starting at day 0 (Δ) or day 38 (▲) or with 100 μl of PBS (●) for controls. After 60 days of treatment, mice were sacrificed and tumor were then fixed. The development of tumors was followed by caliper measurement. Data are the means ± SE of 6 tumors in each group. ***p < 0.001 versus control.

29467942
IHC
H&E staining; 

PubMed: 26943473     


Effect of dual orexin receptor antagonist on sleep and growth plate morphology. (B) Growth plate stained with hematoxylin and eosin.

OX1R / Activated caspase-3; 

PubMed: 29467942     


(B) Indirect immunostaining of OX1R (top) and activated caspase-3 (bottom) in xenografted AsPC-1 tumors resected from nude mice. After necropsy, tumors from nude mice treated by almorexant were resected and paraformaldehyde-fixed and then were cut and used for immunohistochemistry.

26943473 29467942
Immunofluorescence
NPY / ORX-A; 

PubMed: 27727245     


(2) Representative images of ORX-A and NPY immunoreactivity in the PVTN of PSS-exposed rats treated with either vehicle (i), BIBO3304 (ii), mifepristone (iii) or almorexant (iv) before modafinil injection. Images were acquired at a × 10 magnification. Scale bar, 200 μm. The cells in green are NPY-positive and the cells in red are ORX-A-positive. Almorexant and BIBO3304 downregulated the immunoreactivity of ORX-A, ORX-B and NPY fibers and cells in the PVN, ARC, PVTN and PeF.

BDNF / NPY; 

PubMed: 32066707     


(2) A schematic drawing representing the PVN region from which measurements were collected. d The quantitative morphometric analysis of BDNF immunoreactivity (ir) (in area/50,000 mm2) in the PVN 8 days post PSS exposure in exposed rat treated with ACSF (di), ORX-A (dii), or almorexant (diii). e The quantitative morphometric analysis of NPY immunoreactivity (ir) (in area/50,000 mm2) in the PVN 8 days post PSS exposure in exposed rat treated with ACSF (ei), ORX-A (eii), or almorexant (eiii). ACSF artificial cerebrospinal fluid, ALMO almorexant, ASR acoustic startle response, BDNF brain-derived neurotrophic factor, EPM elevated plus maze, NPY neuropeptide Y, ORX orexin, PSS predator-scent stress, PVN paraventricular nucleus of hypothalamus.

27727245 32066707
Representative autoradiograms
LC / TMN / DRN; 

PubMed: 22768296     


Time-course of HCRT1R and HCRT2R occupancies by almorexant. (A,B) Representative autoradiograms showing [3H]SB-674042 (5 nM) binding to HCRTR1 (A) and [3H]EMPA (1 nM) binding to HCRTR2 (B) in rat coronal brain sections. For both receptors, total binding (TB) was maximal in control animals (not injected) sampled at time 0 (t0). For HCRTR1 (A), a clear signal was evident in the locus coeruleus (LC), which could be displaced by co-incubation with an excess of cold SB-674042 (10 µM) (non-specific binding, NSB). In contrast to vehicle administration (Veh, 2 h), almorexant (30 mg/kg injected intraperitoneally at ZT18) attenuated such specific signal after 2 h (Almo, 2 h), but not after 12 h (Almo, 12 h). For HCRTR2 (B), signal was observed in various brain regions, including the tuberomammillary nuclei (TMN), cerebral cortex (CC), field CA3 of the hippocampus (CA3), retrosplenial cortex (RSC), dorsal raphe nuclei (DRN), pontine nuclei (Pn) and parabigeminal nuclei (PBG). [3H]EMPA could be displaced by co-incubation with an excess of Cp5 (10 µM) (NSB). HCRTR2 binding became minimal 2 h after almorexant (Almo, 2 h), but not after Vehicle (Veh+2 h), administration. After 12 h (Almo, 12 h), HCRTR2 binding was intermediate. Scale bars, 2 mm.

22768296
体内研究 Almorexant (300毫克/千克,口服)降低雄性Wistar大鼠的警觉,并增加其非REM和REM睡眠期的电生理学指标。在狗体内,Almorexant (100 毫克/千克,口服)引起嗜睡,并增加REM睡眠的替代标志。[1] Almorexant诱导强的抗抑郁样作用和独立于神经作用与压力相关的下丘脑缺陷的恢复。[2]此外,Almorexant也能降低乙醇自身给药,在高饮用啮齿动物模型中。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1]
- 合并
  • Animal Models: Wistar 大鼠
  • Dosages: ~300 毫克/千克
  • Administration: 口服给药
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 72 mg/mL (131.14 mM)
Water Insoluble
Ethanol ''51 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+25% β-cyclodextrin in saline
9mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 549.02
化学式

C29H32ClF3N2O3

CAS号 913358-93-7
储存条件 粉状
溶于溶剂
别名 ACT-078573 HCl

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID