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
Ebopiprant (OBE022) is an oral and selective prostaglandin F 2α ( PGF 2α ) receptor antagonist, with K i s of 1 nM, 26 nM for human and rat FP receptors, respectively.
In Vitro
Ebopiprant (OBE022) and OBE002 are assayed for FP binding affinity by competitive binding analysis with 3H-PGF2α using HEK293 cells stably transfected with the FP receptor. Binding affinities (K i ) of OBE022 for the human and rat FP receptor are 1 nM and 26 nM respectively. For OBE002, K i s are 6 nM for the human and 313 nM for the rat FP receptor. The binding of both OBE022 and OBE002 is reversible and competitive since increasing concentrations of either compound causes successive decreases in the slope of the binding curves, consistent with an increase in equilibrium dissociation constant (K D ) without a reduction in receptor density. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Time-course of the cumulative percentage of delivers mice after RU486-induced preterm parturition at GD17, in OBE022, nifedipine or vehicle treatment groups. Oral treatment with OBE022 delays the preterm birth caused by RU486 administration as reflected by a shift to the right of the percentage of delivery curve. The effect of oral treatment with nifedipine is comparable. Both OBE022 and nifedipine show a trend to increase the time of first pup delivery. As an important consequence of the prolongation of gestation, dams deliver viable pups. Combination of OBE022 and nifedipine cause a synergistic effect on the delay of RU486-induced preterm birth as reflected by a more pronounced shift to the right of the percentage of delivery curve, in comparison to OBE022 or nifedipine alone. Also, a larger increase of the time of first pup delivery is observed . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Human FP Receptor 1 nM (Ki) Rat FP Receptor 26 nM (Ki)
规格
别名
埃博匹兰
规格或纯度
10mM in DMSO
英文名称
Ebopiprant
生化机理
Ebopiprant （OBE022）是一种口服选择性前列腺素 F 2α （PGF 2α）受体拮抗剂，对人类和大鼠 FP 受体的 K i 分别为 1 nM 和 26 nM。
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
小分子
Isomeric SMILES
CC(C)[C@@H](C(=O)OCC[C@@H](C1=CC=C(C=C1)F)NC(=O)[C@H]2N(CCS2)S(=O)(=O)C3=CC=C(C=C3)C4=CC=CC=C4)N
关联CAS
PubChem CID
MeSH Entry Terms
(S)-2-amino-3-methyl-butyric acid (S)-3-(((S)-3-(biphenyl-4-sulfonyl)-thiazolidine-2-carbonyl)-amino)-3-(4-fluoro-phenyl)-propyl ester;obe022
分子量
599.74
技术文档
高级数据
关联靶点（人）
PTGFR
Tclin
前列腺素 F2-α 受体(Prostaglandin F2-alpha receptor)
(1 活性数据)
安全和危险性（GHS）
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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