欢迎访问ProbeChem中文网站，英文网站请访问www.probechem.com
    英文 |     中文

产品咨询: sales@probechem.com
订购: order@probechem.com

首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-CVN45502
CVN45502

Chemical Structure : CVN45502

CAS No.: 1803556-98-0

加入收藏

CVN45502 (CVN 45502)

货号: PC-21731Not For Human Use, Lab Use Only.

CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).

规格 价格 库存 数量
50 mg Get quote
100 mg Get quote
200 mg Get quote
1 g Get quote
获取报价单
* 请选择数量再加入购物车
 or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).
CVN45502 displays 1000-fold selectivity over human Hcrtr2 receptor (pKi=4.66), CVN45502 (10 µM) also does not engage a broad panel of 125 receptors, ion channels, enzymes and transporters.
CVN45502 is highly brain penetrant with a concentration in the brain of 1.1 ± 0.17 µM 30 minutes after a 3 mg/kg dose and a brain to plasma ratio of 0.7 at 30 minutes and 0.9 at 60 minutes.
CVN45502 fully inhibits the intracellular calcium released in cells expressing Hcrtr1 in response to orexin A with IC50 of 0.02 uM.
CVN45502 (30 mg/kg) ameliorates energy-balance defects after DIO in mice, does not show an alteration of total sleep time or locomotor activity.
CVN45502 (30 mg/kg) leads to a reduction in food intake with no major changes in energy expenditure in leptin deficient genetic obese ob/ob mice.

物理化学性质&存储条件

分子量 432.41
分子式 C19H19F3N8O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((1S,2S)-2-methyl-2-((5-(trifluoromethyl)pyrazin-2-yl)amino)cyclopentyl)-3-(2H-1,2,3-triazol-2-yl)picolinamide

参考文献

1. Marc Schneeberger, et al. Nat Metab. 2022 Nov;4(11):1495-1513.

2. Fieldhouse, C., et al. US patent US-10011588-B2 (2018)

备案号：沪ICP备16042516号-1 Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

联系我们 sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

询单

  • *产品名称:
  • *姓名:
  • *邮箱:
  • *公司名称:
  • *询单数量:
  • *国籍:
  • 询单信息: