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Search Results for " prostaglandin e2 (pge2) "

20

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T83779	EP4 Antagonist 14 Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14
	EP4 antagonist 14是一种前列腺素E2（PGE2）受体亚型EP4的拮抗剂，其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募（IC50 = 0.9 nM）。EP4 antagonist 14（10 µM）能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达，这些mRNA编码Il-4、巨噬细胞甘露糖受体1（Mrc1）、几丁质酶样蛋白3（Chil3）、趋化因子（C-X-C）基序配体1（Cxcl1）、表达在髓样细胞上的触发受体2（Trem2）和精氨酸酶-1（Arg1）。在体内，EP4 antagonist 14（每天30 mg/kg），结合抗PD-1抗体，能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。
T15259	Evatanepag CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Evatanepag (CP-533536 free acid) 是一种 EP2 受体选择性前列腺素 E2 (PGE2) 激动剂，可诱导局部骨形成，EC50 为 0.3 nM。它在大鼠骨折愈合模型中以单剂量局部给药时表现出愈合骨折的能力。
T35610	2,5-dimethyl Celecoxib	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。
T27981	MB-28767 M&B 28767,MB28767
	MB-28767 is an agonist of prostaglandin E2 (PGE2) receptor.
T36168	8-iso-16-cyclohexyl-tetranor Prostaglandin E2 8-iso-16-cyclohexyl-tetranor Prostaglandin E2
	8-iso Prostaglandin E2 (8-iso PGE2) is one of several isoprostanes produced from polyunsaturated fatty acids during lipid peroxidation. 8-iso-16-cyclohexyl-tetranor PGE2 is a synthetic analog of 8-iso PGE2. There are no published studies on the pharmacological properties of 8-iso-16-cyclohexyl-tetranor PGE2.
T36728	9-deoxy-9-methylene Prostaglandin E2 9-deoxy-9-methylene Prostaglandin E2
	9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2 . 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2.
T37839	20-hydroxy Prostaglandin E2 20-hydroxy Prostaglandin E2
	20-hydroxy Prostaglandin E2 (20-hydroxy PGE2) is a product of cytochrome P450 metabolism of PGE2 . ω-Oxidation at C-20 followed by β-oxidation and the loss of up to four carbons from the lower side chain is a prominent metabolic pathway for PGE2. 20-hydroxy PGE2 is the putative first intermediate in this chain of chemical transformations.
T69755	Evatanepag sodium
	Evatanepag, also known as CP-533536, is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.
T38342	11-deoxy Prostaglandin E2 11-deoxy Prostaglandin E2
	11-deoxy Prostaglandin E2 (11-deoxy PGE2) is a stable, synthetic analog of PGE2 . In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and contracts human respiratory tract smooth muscle with potencies ranging from 5 to 30 times higher than PGF2α .
T38305	tetranor-PGAM
	Prostaglandin E2 (PGE2), one of the most widely investigated PGs, can be used as a biomarker of inflammation, disease state, or therapeutic effectiveness. However due to its rapid metabolism, direct measurement of PGE2 in biological samples is difficult. The major urinary metabolite of PGE2, tetranor-PGEM, serves as an indirect marker of PGE2 biosynthesis. Though like PGE2, tetranor-PGEM is also chemically unstable. tetranor-PGAM is a dehydration product of tetranor-PGEM and can be measured as a...
T36829	9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2 9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2
	9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2 (Meteneprost) is a potent analog of prostaglandin E2 with an extended half-life in vivo. In combination with various other prostaglandin derivatives, it results in the termination of first trimester pregnancy in monkeys. A single intramuscular injection containing 0.5 mg of meteneprost and 7.5 mg of 17-phenyl trinor PGF1α is very effective in terminating early pregnancy. This prostaglandin mixture is ineffective on monkeys in their third trimes...
T36045	1a,1b-dihomo Prostaglandin E2 1a,1b-dihomo Prostaglandin E2
	1a,1b-dihomo Prostaglandin E2 (PGE2) is a rare polyunsaturated fatty acid first identified in extracts of sheep vesicular gland microsomes, known to contain COX, incubated with adrenic acid . 1a,1b-dihomo PGE2 has also been identified in conditioned media of RAW 264.7 macrophages stimulated with endotoxin and arachidonic acid . This product is thought to be produced by elongation of AA to adrenic acid, which is then metabolized sequentially by COX and PGE synthase.
T35991	ent-Prostaglandin E2 ent-Prostaglandin E2
	Enzymatically-derived prostaglandin E2 (PGE2) is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings of oxidative stress via the isoprostane pathway. A proposed mechanism for the formation of rac-PGE2 involves the base catalyzed equilibration from 15-E2t-isoprostane (8-iso-PGE2), g...
T37918	Prostaglandin E2 isopropyl ester Prostaglandin E2 isopropyl ester
	Prostaglandin E2 (PGE2) isopropyl ester is a more lipophilic form of the free acid, PGE2. PG esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid by endogenous esterases upon in vivo administration, making the esters useful prodrugs. In general, the C-1 esters of PGs show greatly diminished receptor activity in vitro compared to the parent free acids.
T83773	Prostaglandin E2 Inhibitor 3 PGE2 Inhibitor 3
	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。
T22172	YS-121
	YS121 是微粒体前列腺素 E2 合酶-1 (mPGES-1;IC50=3.4 μM) 和 5-脂氧合酶 (5-LOX;IC50=6.5 μM) 的双重抑制剂。在 IL-1β 刺激的 A549 细胞中，YS121以剂量依赖性地方式减少 PGE2 的产生，EC50为 12 μM。
T68738	(±)-γ-Tocopherol
	(±)-γ-Tocopherol is a form of vitamin E with antioxidant and anti-inflammatory properties. It traps and detoxifies reactive nitrogen oxide species, including nitrogen dioxide, in cell-free assays. It also reduces the synthesis of prostaglandin E2 (PGE2) induced by LPS in RAW 264.7 macrophages and by IL-1β in A549 cells. (±)-γ-Tocopherol inhibits LPS-induced nitrite release and inducible nitric oxide synthase (iNOS) expression in RAW 264.7 cells and reduces COX-2 activity in A549 cells pretreated...
T83785	2-Chloroadenosine-5'-O-diphosphate sodium 2-chloro ADP
	2-Chloroadenosine-5'-O-diphosphate是一种腺苷5'二磷酸（ADP）的衍生物。它在浓度依赖性的方式下，促进了人类富含血小板的血浆中的聚集，并抑制了由前列腺素E2（PGE2）诱导的环磷酸腺苷（cAMP）的产生。2-Chloroadenosine-5'-O-diphosphate引起预收缩的孤立的豚鼠taenia coli条带放松（pD2 = 6.74），降低大鼠的动脉血压。此外，它还抑制了热休克蛋白70（Hsp70）家族成员mortalin的ATP酶活性（人类酶的表观Ki = 45.05 µM）。
T37441	KMN-80
	The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other pro...
T82805	Butaprost free acid
	(R)-Butaprost (free acid) 是PGE2的一个结构类似物，特异性地对EP2受体亚型有选择性。该化合物用于药理学研究，以确定不同人类及动物组织和细胞中EP受体的分布。去除甲酯基团并恢复C-1自然羧酸后，增强了(R)-butaprost与前列腺素受体的结合亲和力，通常情况下，游离酸形式的亲和力是相应酯形式的10到100倍。尽管(R)-butaprost作为C-16的较低活性差向异构体，其药理作用未经充分研究，但在1986年Gardiner的论文中提到的TR 4979即布他前列素，结构中的差向异构体错误表达为16(R)，实际为16(S)，该错误直至1990年代后期才被美国和日本的研究纠正。

化合物

EP4 Antagonist 14

Cat.No: T83779

Synonym: Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14

Cat.No: T15259

Synonym: CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸

Target: Prostaglandin Receptor

2,5-dimethyl Celecoxib

Cat.No: T35610

Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor

Cat.No: T27981

Synonym: M&B 28767,MB28767

8-iso-16-cyclohexyl-tetranor Prostaglandin E2

Cat.No: T36168

Synonym: 8-iso-16-cyclohexyl-tetranor Prostaglandin E2

9-deoxy-9-methylene Prostaglandin E2

Cat.No: T36728

Synonym: 9-deoxy-9-methylene Prostaglandin E2

20-hydroxy Prostaglandin E2

Cat.No: T37839

Synonym: 20-hydroxy Prostaglandin E2

Evatanepag sodium

Cat.No: T69755

11-deoxy Prostaglandin E2

Cat.No: T38342

Synonym: 11-deoxy Prostaglandin E2

Cat.No: T38305

9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2

Cat.No: T36829

Synonym: 9-deoxy-9-methylene-16,16-dimethyl Prostaglandin E2

1a,1b-dihomo Prostaglandin E2

Cat.No: T36045

Synonym: 1a,1b-dihomo Prostaglandin E2

ent-Prostaglandin E2

Cat.No: T35991

Synonym: ent-Prostaglandin E2

Prostaglandin E2 isopropyl ester

Cat.No: T37918

Synonym: Prostaglandin E2 isopropyl ester

Prostaglandin E2 Inhibitor 3

Cat.No: T83773

Synonym: PGE2 Inhibitor 3

Cat.No: T22172

(±)-γ-Tocopherol

Cat.No: T68738

2-Chloroadenosine-5'-O-diphosphate sodium

Cat.No: T83785

Synonym: 2-chloro ADP

Cat.No: T37441

Butaprost free acid

Cat.No: T82805

Cat. No.	Product Name	Target	Signaling Pathways
T5014	Prostaglandin E2 地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2)	Endogenous Metabolite; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism
	Prostaglandin E2 (PGE2) 是一种天然激素，参与人体内的各种生理过程，包括平滑肌收缩和放松、调节血管扩张和收缩、调节血压和炎症调节。
TN2091	Polygalacin D	Apoptosis; IAP	Apoptosis
	Polygalacin D 是从桔梗中分离的一种天然产物，具有抗癌和抗增殖特性。它通过 PI3K/Akt 途径诱导凋亡。它抑制 IAP 蛋白家族的表达，并通过抑制 GSK3β，Akt 的磷酸化和 PI3K 的表达来阻断 PI3K/Akt 途径。
T3926	Echinatin 刺甘草查尔酮,Retrochalcone	Free radical scavengers	oxidation-reduction
	Echinatin (Retrochalcone) 是分离自中草药甘草中，具有保肝和抗炎活性。在大鼠中，它可以被快速吸收和消除，并广泛分布，绝对生物利用度约为 6.81％。
TN1871	Ligustroside	EGFR; Lipoxygenase; COX	Angiogenesis; Immunology/Inflammation; JAK/STAT signaling; Metabolism; Neuroscience; Tyrosine Kinase/Adaptors
	Ligustroside shows little antioxidant, and anti-inflammatory properties, it shows a significant inhibition effect on prostaglandin E2 (PGE2)-release. Ligustroside shows moderate antiviral activities against parainfluenza type 3 virus.

天然产物

Prostaglandin E2

Cat.No: T5014

Synonym: 地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2)

Target: Endogenous Metabolite, Prostaglandin Receptor

Cat.No: TN2091

Target: Apoptosis, IAP

Cat.No: T3926

Synonym: 刺甘草查尔酮,Retrochalcone

Target: Free radical scavengers

Cat.No: TN1871

Target: EGFR, Lipoxygenase, COX

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