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Cat. No. | Product Name | Target | Signaling Pathways |
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T2681 |
hPGDS-IN-1
|
PGE Synthase | Immunology/Inflammation |
hPGDS-IN-1是 hPGDS 抑制剂,使用荧光偏振检测或通过 EIA 法测得的 IC50值为12 nM。 | |||
T1804 |
HPGDS inhibitor 1
HPGDS-inhibitor-1 |
PGE Synthase | Immunology/Inflammation |
HPGDS inhibitor 1 是口服具有活性的HPGDS 选择性抑制剂,在酶和细胞分析中的IC50值分别为 0.6 nM 和 32 nM,但对 L-PGDS、mPGES、COX-1、COX-2 、5-LOX 无抑制作用。 | |||
T10098 |
PGS-IN-1
KME-4 |
Lipoxygenase; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism |
PGS-IN-1 (KME-4)是一种前列腺素合成酶抑制剂,IC50=0.28 μM。它也可抑制5-脂肪氧合酶的活性,IC50=1.05 μM。 | |||
T37778 |
19(R)-hydroxy Prostaglandin E1
19(R)-hydroxy Prostaglandin E1 |
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19(R)-hydroxy Prostaglandin E1 是 EP1 和 EP3 受体亚型的激动剂,并对平滑肌表现出收缩活性,也是灵长类动物精液中的主要前列腺素。 | |||
T36147 |
13,14-dihydro-15-keto Prostaglandin E1
13,14-dihydro-15-keto Prostaglandin E1 |
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13,14-dihydro-15-keto Prostaglandin E1 可抑制 ADP 诱导的人离体富血小板血浆中的血小板聚集(IC50=14.8 μg/mL),也是 PGE1 代谢物。 | |||
T23861 |
CAY10526
CAY-10526,BTH,CAY 10526 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂,可抑制 NF-κB 信号通路。 | |||
T15757 |
Limaprost
17α,20-dimethyl-δ2-PGE1,利马前列素,OP1206,ONO1206 |
PGE Synthase | Immunology/Inflammation |
Limaprost (17α,20-dimethyl-δ2-PGE1) 是PGE1类似物,也是口服具有活性的血管舒张剂。它能够增加血流量以及减少血小板聚集。它具有抗心绞痛的功能,可用于疼痛的缓解,以及用于研究缺血性症状。 | |||
T28089 |
mPGES-1 Inhibitor-1
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
mPGES-1 Inhibitor-1 是一种新型的微粒体前列腺素 E 合酶-1(mPGES-1)选择性抑制剂,具有抗炎镇痛活性,可用于研究急性肝损伤。 | |||
T21738 |
PF-9184
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-9184 是一种有效且高度选择性的人微粒体前列腺素 E 合酶 1 (mPGES-1) 的抑制剂,IC50 值为 16.5 nM。PF-9184 体外抑制 IL-1β 诱导的 PGE2 合成。 | |||
T35610 |
2,5-dimethyl Celecoxib
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Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor | Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells |
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。 | |||
T79846 |
Friluglanstat
|
PGE Synthase | Immunology/Inflammation |
Friluglanstat为一种mPGES-1抑制剂,表现出抗炎作用。 | |||
T39000 |
Zaloglanstat
GRC-27864,ISC-27864 |
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Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases. | |||
T16504 |
PF-4693627
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Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA). | |||
T36887 |
8(E),10(E),12(Z)-Octadecatrienoic Acid
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8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland... | |||
T74781 |
UT-11
|
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UT-11是一种有效且具有脑渗透性的mPGES-1抑制剂,能够降低人类(SK-N-AS)和小鼠(BV2)细胞内PGE2的生成,其IC50s分别是0.10 μM和2.00 μM。 | |||
T26925 |
Butaprost
Butaprostum,TR-4979,(R)-Butaprost |
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Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3]. | |||
T68334 | AF3442 | ||
AF3442 is a potent and selective mPGES-1 inhibitor (microsomal prostaglandin (PG) E synthase-1). AF3442 caused a concentration-dependent inhibition of PGE(2) in human recombinant mPGES-1 with an IC(50) of 0.06microM. AF3442 is a selective mPGES-1 inhibitor which reduced monocyte PGE(2) generation also in the presence of plasma proteins. Pharmacological inhibition of mPGES-1 did not translate into redirection of PGH(2) metabolism towards other terminal PG synthases in monocytes. The functional re... | |||
T83773 |
Prostaglandin E2 Inhibitor 3
PGE2 Inhibitor 3 |
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Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂,相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH),在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下,该抑制剂能抑制A549细胞中IL-1β诱导的PGE2生成以及在J774A.1巨噬细胞中,LPS诱导的IL-6和PGE2生成。同时,它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成,包括白三烯B4 (LTB4) 和5-H(p)ETE(IC50s分别为4.9和5.2 µM)。在体内,10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。 | |||
T35961 |
Prostaglandin Bx
|
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PGBx is a mixture of oligomers of PGB1 with a molecular weight of 1,000-1,500. It has antioxidant and free radical trapping activity that was first studied in isolated mitochondria.1 PGBx has anti-inflammatory and cytoprotective activity which may be attributed to inhibition of the 14 kDa sPLA2.2,3 At a dose of 1 mg/kg, PGBx significantly reduces the incidence of ulcers in rats.2References1. Polis, B.D., Polis, E., and Kwong, S. Protection and reactivation of oxidative phosphorylation in mitocho... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T1626 |
Prostaglandin E1
前列地尔,PGE1,列腺素E1,Alprostadil |
Endogenous Metabolite; Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism |
Prostaglandin E1 (Alprostadil) 是一种前列腺素受体配体,对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集,可作为血管扩张剂用于外周血管疾病的研究。 | |||
T6S1027 |
Tussilagone
|
Others | Others |
Tussilagone 是Tussilago farfara 的主要活性成分,具有抗炎作用。它抑制盲肠结扎和穿刺导致脓毒症的小鼠的炎症反应,提高其生存率。它改善葡聚糖硫酸钠诱导的小鼠结肠炎的炎症反应。 |