计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC 50 of 15.3 nM for human EP4-R . BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research
In Vitro
BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BAY-1316957 (Compound 32; 0.2-5 mg/kg; oral administration; once) treatment significantly reduces mechanical allodynia in dmPGE2 pain model . The pharmacokinetic parameters of BAY-1316957 (Compound 32) shows a low clearance, long half-life, and high bioavailability (F%=90%) in Wistar rats. Investigation of the metabolic pathways of BAY-1316957 (Compound 32) in human, rat, mouse, dog, and monkey hepatocytes revealed that the formation of the acyl glucuronide was also the common and predominant route of biotransformation, mainly catalyzed by UGT1A1 and to a lesser extent by UGT1A3 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male adult Sprague Dawley rats (220-265 g) injected with 16,16-dimethyl prostaglandin E2 (dmPGE2) Dosage: 0.2 mg/kg, 1 mg/kg, 5 mg/kg Administration: Oral administration; once Result: Significantly reduced paw withdrawal thresholds in dmPGE2 pain model.
IC50& Target:human EP4-R 15.3 nM (IC 50 )
规格
别名
海湾-1316957
规格或纯度
10mM in DMSO
英文名称
BAY-1316957
生化机理
BAY-1316957 是一种强效、选择性和口服活性的前列腺素 E2 受体亚型 4（EP4-R）拮抗剂，对人类 EP4-R 的 IC 50 为 15.3 nM。BAY-1316957 具有良好的药物代谢和药代动力学特性，可用于治疗子宫内膜异位症。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
未知
Isomeric SMILES
CCN1C2=C(C=C(C=C2)C)C3=C1C=CC(=C3)C4=NC5=C(N4CCOC)C=CC(=C5C)C(=O)O
PubChem CID
分子量
441.52
技术文档
高级数据
关联靶点（人）
PTGER4
Tclin
前列腺素 E2 受体 EP4 亚型(Prostaglandin E2 receptor EP4 subtype)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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