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-Prostaglandin Receptor-OC000459
OC000459

Chemical Structure : OC000459

CAS No.: 851723-84-7

加入收藏

OC000459 (Timapiprant)

货号: PC-38844Not For Human Use, Lab Use Only.

OC000459 is a potent, selective, and orally active D prostanoid receptor 2 (DP2, CRTH2) antagonist with Ki of 13/3 nM for human/recombinant DP2, respectively.

规格 价格 库存 数量
10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2280 In stock
100 mg 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) Select Batch:

生物&药学活性

OC000459 (Timapiprant) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, CRTH2) antagonist with Ki of 13/3 nM for human/recombinant DP2, respectively.
OC000459 does not interfere with the ligand binding properties or functional activities of other prostanoid receptors (prostaglandin E1-4 receptors, D1, thromboxane receptor, prostacyclin receptor, and prostaglandin F receptor).
OC000459 inhibited chemotaxis (IC50= 28 nM) of human Th2 lymphocytes and cytokine production (IC50=19 nM) by human Th2 lymphocytes.
OC000459 competitively antagonized eosinophil shape change responses induced by PGD₂ in both isolated human leukocytes (pK(B)=7.9) and human whole blood (pK(B)=7.5) but did not inhibit responses to eotaxin, 5-oxo-eicosatetraenoic acid, or complement component C5a.
OC000459 is orally bioavailable in rats and effective in inhibiting blood eosinophilia induced by 13,14-dihydro-15-keto-PGD₂ (DK-PGD₂) with ED50 of 0.04 mg/kg (p.o.) and airway eosinophilia in response to an aerosol of DK-PGD₂ in guinea pigs (ED50=0.01 mg/kg p.o.).

物理化学性质&存储条件

分子量 348.377
分子式 C21H17FN2O2
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

5-fluoro-2-methyl-3-(2-quinolinylmethyl)-1H-indole-1-acetic acid

参考文献

1. Pettipher R, et al. J Pharmacol Exp Ther. 2012 Feb;340(2):473-82.

2. Barnes N, et al. Clin Exp Allergy. 2012 Jan;42(1):38-48.

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: