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Search Results for " prostaglandin e 2 "

28

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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.
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.
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.
T36161	8-iso Prostaglandin E2 isopropyl ester 8-iso Prostaglandin E2 isopropyl ester
	8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the C-1 esters of prostaglandins show greatly diminished agonist activity in vitro compared to the parent free acids.
T37996	17-phenyl trinor Prostaglandin E2 ethyl amide 17-phenyl trinor Prostaglandin E2 ethyl amide
	17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to inc...
T7948	HPGDS inhibitor 2 GSK-2894631A	PGE Synthase	Immunology/Inflammation
	HPGDS inhibitor 2 (GSK-2894631A) 是高效的造血前列腺素 D 合成酶(H-PGDS)选择性抑制剂(IC50:9.9 nM)。
T36144	11β-Prostaglandin E2 11β-PGE2,11β-Prostaglandin E2
	11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM.[1] 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2.2 11β-PGE2 inhibits PGE2 binding to the prostaglandin transporter protein with a Ki of 56 nM.[3] .
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.
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 .
T36160	8-iso Prostaglandin E2 8-iso Prostaglandin E2
	8-iso PGE2 is one of several isoprostanes produced from arachidonic acid during lipid peroxidation. It is a potent renal vasoconstrictor in the rat. 8-iso PGE2 inhibits U-46619 or I-BOP-induced platelet aggregation with IC50 values of 0.5 and 5 μM, respectively. When infused into the renal artery of the rat at a concentration of 4 μg/kg/min, 8-iso PGE2 decreases the GFR and renal plasma flow by 80% without affecting blood pressure.
T36154	15(S)-15-methyl Prostaglandin E2 15(S)-15-methyl Prostaglandin E2
	15(S)-15-methyl PGE2 is a potent, metabolically stable analog of PGE2. It is a potent gastric antisecretory and antiulcer compound. 15(S)-15-methyl PGE2 binds to human myometrium with twice the affinity of PGE2 and is ten times more potent than PGE1 in contracting uterine smooth muscle.
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。
T78582	15-keto-Prostaglandin E2 15-keto-PGE2	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	15-keto-Prostaglandin E2为内源性代谢产物，通过与STAT3Cys259残基结合，抑制STAT3激活作用。该化合物能够结合并稳定EP2与EP4受体，进而抑制乳腺癌细胞生长与进展，并通过激活PPAR-γ促进真菌生长。
T71851	5-trans-Prostaglandin E2
	5-trans-Prostaglandin E2 accelerates fibrinolysis by enhancing plasminogen activation mediated by tissue-type plasminogen activator. It also inhibits platelet aggregation in human PRP.
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.
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...
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。
T13488	2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide 2-_E-2-decenoylamino_ethyl_2-_cyclohexylethyl__sulfide	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound known to inhibit stress-induced ulcers, effectively maintaining the levels of phospholipase A2 and prostaglandin E2 in rats subjected to water immersion-restrained stress-induced ulceration.
T36887	8(E),10(E),12(Z)-Octadecatrienoic Acid
	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...
T68904	GW-833972A free base
	GW833972 is a CB2 Agonist. GW 833972A inhibited capsaicin-induced depolarization of the human and guinea-pig and prostaglandin E(2) (PGE(2)) and hypertonic saline-induced depolarization of the guinea-pig isolated vagus nerve in vitro. GW 833972A also inhibited citric acid-induced cough but not plasma extravasation in the guinea-pig and this effect was blocked by a CB(2) receptor antagonist.
T26925	Butaprost Butaprostum,TR-4979,(R)-Butaprost
	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...
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...
T37213	5-trans Latanoprost
	Latanoprost is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. 5-trans Latanoprost is an isomer of latanoprost wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity of between 2-5% in most commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. Fr...
T36165	8-iso-13,14-dihydro-15-keto Prostaglandin F2α 8-iso-13,14-dihydro-15-keto Prostaglandin F2α
	8-iso-13,14-dihydro-15-keto Prostaglandin F2α (8-iso-13,14-dihydro-15-keto PGF2α) is a metabolite of the isoprostane, 8-isoprostane (8-iso PGF2α), in rabbits, monkeys and humans. 8-iso PGF2α is a PG-like product of non-specific lipid peroxidation. In both humans and monkeys, exogenously infused 8-isoprostane is converted primarily to metabolites having 2 or 4 carbon atoms removed from the top side chain by β-oxidation. A similar pattern is observed when tritiated 8-isoprostane is infused into ra...
T35961	Prostaglandin Bx
	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...
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...

化合物

ent-Prostaglandin E2

Cat.No: T35991

Synonym: ent-Prostaglandin E2

Prostaglandin E2 isopropyl ester

Cat.No: T37918

Synonym: Prostaglandin E2 isopropyl ester

1a,1b-dihomo Prostaglandin E2

Cat.No: T36045

Synonym: 1a,1b-dihomo Prostaglandin E2

9-deoxy-9-methylene Prostaglandin E2

Cat.No: T36728

Synonym: 9-deoxy-9-methylene Prostaglandin E2

8-iso Prostaglandin E2 isopropyl ester

Cat.No: T36161

Synonym: 8-iso Prostaglandin E2 isopropyl ester

17-phenyl trinor Prostaglandin E2 ethyl amide

Cat.No: T37996

Synonym: 17-phenyl trinor Prostaglandin E2 ethyl amide

HPGDS inhibitor 2

Cat.No: T7948

Synonym: GSK-2894631A

Target: PGE Synthase

11β-Prostaglandin E2

Cat.No: T36144

Synonym: 11β-PGE2,11β-Prostaglandin E2

20-hydroxy Prostaglandin E2

Cat.No: T37839

Synonym: 20-hydroxy Prostaglandin E2

11-deoxy Prostaglandin E2

Cat.No: T38342

Synonym: 11-deoxy Prostaglandin E2

8-iso Prostaglandin E2

Cat.No: T36160

Synonym: 8-iso Prostaglandin E2

15(S)-15-methyl Prostaglandin E2

Cat.No: T36154

Synonym: 15(S)-15-methyl Prostaglandin E2

Prostaglandin E2 Inhibitor 3

Cat.No: T83773

Synonym: PGE2 Inhibitor 3

15-keto-Prostaglandin E2

Cat.No: T78582

Synonym: 15-keto-PGE2

Target: Prostaglandin Receptor

5-trans-Prostaglandin E2

Cat.No: T71851

8-iso-16-cyclohexyl-tetranor Prostaglandin E2

Cat.No: T36168

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

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

Cat.No: T36829

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

2,5-dimethyl Celecoxib

Cat.No: T35610

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

2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide

Cat.No: T13488

Synonym: 2-_E-2-decenoylamino_ethyl_2-_cyclohexylethyl__sulfide

Target: Prostaglandin Receptor

8(E),10(E),12(Z)-Octadecatrienoic Acid

Cat.No: T36887

GW-833972A free base

Cat.No: T68904

Cat.No: T26925

Synonym: Butaprostum,TR-4979,(R)-Butaprost

Cat.No: T68334

(±)-γ-Tocopherol

Cat.No: T68738

5-trans Latanoprost

Cat.No: T37213

8-iso-13,14-dihydro-15-keto Prostaglandin F2α

Cat.No: T36165

Synonym: 8-iso-13,14-dihydro-15-keto Prostaglandin F2α

Prostaglandin Bx

Cat.No: T35961

Cat.No: T37441

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。
T2S0765	Epibetulinic acid	NO Synthase; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Epibetulinic acid 对细菌内毒素刺激的小鼠巨噬细胞 (RAW 264.7) 中 NO 和前列腺素 E(2) 的产生具有有效的抑制作用，IC50分别为 0.7 和 0.6 μM，具有抗炎活性。
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。
TN4959	Schizandriside	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Schizandriside may have anti-inflammatory effects, it has inhibitory activities against nitric oxide and prostaglandin E(2) production in IFN-γ- and lipopolysaccharide-stimulated RAW 264.7 cells. It shows significant cytotoxicity against A549, SK-OV-3, SK

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

Epibetulinic acid

Cat.No: T2S0765

Target: NO Synthase, Prostaglandin Receptor

Cat.No: T6S1027

Target: Others

Cat.No: TN4959

Target: Prostaglandin Receptor

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