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Key Documents

SML2076

Sigma-Aldrich

ONO-AE3-208

≥98% (HPLC)

同義詞:

4-(4-氰基-2-(2-(4-氟萘-1-基)丙酰胺基)苯基)丁酸, 4-氰基-2-[[[2-(4-氟-1-萘基)-1-氧丙基]氨基]苯丁酸, AE3-208

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About This Item

經驗公式(希爾表示法):
C24H21FN2O3
CAS號碼:
分子量::
404.43
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

CC(C1=C(C=CC=C2)C2=C(F)C=C1)C(NC3=CC(C#N)=CC=C3CCCC(O)=O)=O

InChI

1S/C24H21FN2O3/c1-15(18-11-12-21(25)20-7-3-2-6-19(18)20)24(30)27-22-13-16(14-26)9-10-17(22)5-4-8-23(28)29/h2-3,6-7,9-13,15H,4-5,8H2,1H3,(H,27,30)(H,28,29)

InChI 密鑰

MTDIMKNAJUQTIO-UHFFFAOYSA-N

生化/生理作用

ONO-AE3-208是一种口服活性前列腺素E2受体4(EP4)选择性拮抗剂(nM为单位的Ki = 1.3/EP4,30/EP3,790/FP和2400/TP;针对前列腺素受体DP、EP1、EP2、IP的Ki >10 μM)。EP4-/-小鼠和用ONO-AE3-208处理的野生型小鼠(在饮用水中10 mg/kg /天)都在DSS诱发的肠炎小鼠模型中表现出了严重的症状(腹泻、嗜血、体重减轻)。ONO-AE3-208也被报道可在体内促进胎儿和新生大鼠的动脉导管收缩(口胃给药10 mg/kg)。此外,ONO-AE3-208在体外已展示出可有效抑制1 ng/mL IL-1β诱导的HUVEC迁移(被1或10 μM的AE3-208分别抑制53%和75%),并在体内可阻断IL-1β( 30 ng/Hydron颗粒植入物)诱导的小鼠角膜血管生成(口服1 mg/kg/天)。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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Indomethacin is used to constrict the patent ductus arteriosus in premature infants. To clarify possible prostanoid receptor antagonists that can constrict the ductus, we studied in vivo constriction of the fetal and neonatal ductus arteriosus by AE3-208, a prostanoid EP4-receptor
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Cyclooxygenase1 (COX1) and COX2 mediate the rate-limiting step in arachidonic acid metabolism. Expression of COX2 mRNA and protein is often enhanced in various human cell types by inflammatory cytokines such as interleukin-1beta (IL-1beta) and tumor necrosis factor alpha (TNFalpha). IL-1beta

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