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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
其他客户在看
Kenji Kabashima et al.
The Journal of clinical investigation, 109(7), 883-893 (2002-04-03)
We used mice deficient in each of the eight types and subtypes of prostanoid receptors and examined the roles of prostanoids in dextran sodium sulfate-induced (DSS-induced) colitis. Among the prostanoid receptor-deficient mice, only EP4-deficient mice and not mice deficient in
Kenta Watanabe et al.
Biochemical and biophysical research communications, 478(1), 154-161 (2016-07-28)
The metastasis of tumors to bone is known to be promoted by prostaglandin E2 (PGE2) produced by the tumor host stromal tissue. Although bone metastases frequently occur in prostate cancer patients, the significance of PGE2 in stromal responses to the
Mousumi Majumder et al.
Stem cells (Dayton, Ohio), 34(9), 2290-2305 (2016-06-15)
Cancer stem-like cells (SLC) resist conventional therapies, necessitating searches for SLC-specific targets. We established that cyclo-oxygenase(COX)-2 expression promotes human breast cancer progression by activation of the prostaglandin(PG)E-2 receptor EP4. Present study revealed that COX-2 induces SLCs by EP4-mediated NOTCH/WNT signaling.
Kazuo Momma et al.
Pediatric research, 58(5), 971-975 (2005-11-01)
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
Takashi Kuwano et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 18(2), 300-310 (2004-02-11)
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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