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Search Results for " prostaglandin d2 "

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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T38389	Prostaglandin D2 Ethanolamide Prostaglandin D2 Ethanolamide
	Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of minia...
T36545	Prostaglandin D2 methyl ester Prostaglandin D2 methyl ester
	Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2.
T36153	15(S)-15-methyl Prostaglandin D2 15(S)-15-methyl Prostaglandin D2
	15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2 . In contrast to PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction and increases systemic blood pressure with much reduced inhibitory activity on ADP-induced platelet aggregation. It also exhibits strong antifertility activity in hamsters (200-fold more potent than PGD2).
T37264	15(R)-15-methyl Prostaglandin D2 15(R)15methyl PGD2	GPR	Endocrinology/Hormones; GPCR/G Protein
	15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物，也是一种具有选择性和强效性的 CRTH2/DP2 受体激动剂，可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。
T36213	16,16-dimethyl Prostaglandin D2 16,16-dimethyl Prostaglandin D2
	16,16-dimethyl PGD2 is a metabolically stable synthetic analog of PGD2. It enhances ADP-induced human platelet aggregation and increases systemic blood pressure in rats.
T14211	AMG-009	Others	Others
	AMG-009 is a prostaglandin D2 antagonist. For CRTH2 and DP receptors, the IC50s are 3 nM and 12 nM, respectively.
T16280	Nedocromil FPL 59002,尼多克罗	Leukotriene Receptor; Prostaglandin Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Nedocromil (FPL 59002) 对多种介质的作用或形成有抑制作用，包括组胺，前列腺素 D2和白三烯 C4。
T15712	Laropiprant MK-0524	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Laropiprant (MK-0524) 是 DP receptor 的选择性拮抗剂，Ki 为 0.57 nM，对 TP 受体的 Ki 为 2.95 nM。
T1866	AT-56	Others; PGE Synthase	Immunology/Inflammation; Others
	AT56 是口服有活性的脂钙蛋白型前列腺素 D 合酶 (L-PGDS) 选择性抑制剂，其IC50=95 μM，Ki=75 μM。它能够特异性地抑制L-PGDS 催化的 PGD2介导的嗜睡或疼痛反应。
T7652	AM211 AM211 free acid	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	AM211 (AM211 free acid) 是可口服的选择性前列腺素受体拮抗剂，对人、小鼠、豚鼠和大鼠的 DP2 的IC50值分别为 4.9、7.8、4.9 和 10.4 nM。
T4624	PGD2-IN-1 PGD2-inhibitor	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	PGD2-IN-1 (PGD2-inhibitor) 是一种有效的DP 受体拮抗剂(IC50 : 0.3 nM),是一种可以抑制前列腺素D2 (PGD2)信号传导的化合物。PGD2-IN-1 专门针对和调节PGD2受体或参与PGD2合成或代谢的酶的活性。
T15829	L 888607 Racemate	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	L 888607 Racemate is a selective antagonist of prostaglandin D2 receptor subtype 1 (DP1) (Kis: 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively).
T41073	Pexopiprant
	Pexopiprant, a potent oral antagonist of the prostaglandin D2 receptor 2 (DP2) with a K i value less than 100nM, is a valuable compound for asthma research.
T10891	CRTH2-IN-1 Ramatroban analog	P450	Metabolism
	CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.
T38307	tetranor-PGJM
	Tetranor-PGJM 是前列腺素 D2 的代谢物，与姜黄素发挥抗炎作用相关。
T21869	BW A868C
	BW A868C 是一种乙内酰脲化合物，是 BW245C 结构类似物。BW A868C 是一种选择性强的前列腺素 D2 (PGD2) 竞争性拮抗剂。BW A868C 对其他前列腺素受体 (IP、EP1、EP2、TP 和 FP) 没有影响。
T38365	CAY10597
	The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the...
T73782	Prostaglandin J2
	Prostaglandin J2 (PGJ2) 是前列腺素 D2 (PGD2) 的一种内源性代谢物，是一种有效的 PGD2 受体 (DP) 激动剂，对 hDP 和 hCRTH2 的 Ki 分别为 0.9 nM 和 6.6 nM。Prostaglandin J2 刺激细胞内环 AMP 的产生，EC50值为 1.2 nM。Prostaglandin J2 诱导氧化应激和神经细胞凋亡。Prostaglandin J2 诱导泛素化 (Ub) 蛋白的积累/聚集。Prostaglandin J2 具有高度神经毒性，可导致许多神经退行性疾病，包括阿尔茨海默病 (AD) 和帕金森病 (PD)。
T38257	PGDM
	Prostaglandin D2 (PGD2) plays a pharmacological role in allergic and asthmatic anaphylaxis, normal physiological sleep and lowering of body temperature, as well as inhibits platelet aggregation and relaxes vascular smooth muscle. PGDM is a major urinary metabolite of PGD2 with a unique lower sidechain that readily undergoes reversible cyclization. It is used as a biomarker to assess endogenous production of PGD2.
T71088	AM-211 sodium
	AM-211 sodium is a novel and potent antagonist of the prostaglandin D2 receptor type 2. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it shows selectivity over other prostanoid receptors and enzymes. AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay.
T41267	PROTAC(H-PGDS)-7
	PROTAC(H-PGDS)-7 是一种有选择性的、有效的小分子造血前列腺素 D 合酶（H-PGDS）PROTAC 降解剂，在 KU812细胞中展现出降解活性，DC50为 17.3 pM。PROTAC(H-PGDS)-7是一种类药化合物，能有效抑制前列腺素 D2 (PGD2)的产生，抑制炎症因子重生作用。PROTAC(H-PGDS)-7是治疗 DMD 和其他H-PGDS 相关疾病的候选化合物。
T35811	CAY10410
	CAY10410 is an analog of prostaglandin D2/prostaglandin J2 (PGD2/PGJ2) with structural modifications intended to give it PPARγ ligand activity and resistance to metabolism. 15-deoxy-δ12,14-PGJ2 has been shown to be a potent ligand for PPARγ. Metabolism of the cyclopentenone prostaglandins PGA2, PGJ2, and δ12-PGJ2 occurs via glutathione addition across the α,β unsaturated enone. CAY10410 was designed as an analog of the PPARγ-binding prostaglandins which could not undergo this conjugation reactio...
T38306	tetranor-PGDM
	Prostaglandin D2 is synthesized by hematopoietic-type PGD-synthase (H-PGDS) in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. PGD2 is also produced in the brain by lipocalin-PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. tetranor-PGDM is a major metabolite of PG...
T36418	O-Desmethyl-N-deschlorobenzoyl Indomethacin
	O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism ...

化合物

Prostaglandin D2 Ethanolamide

Cat.No: T38389

Synonym: Prostaglandin D2 Ethanolamide

Prostaglandin D2 methyl ester

Cat.No: T36545

Synonym: Prostaglandin D2 methyl ester

15(S)-15-methyl Prostaglandin D2

Cat.No: T36153

Synonym: 15(S)-15-methyl Prostaglandin D2

15(R)-15-methyl Prostaglandin D2

Cat.No: T37264

Synonym: 15(R)15methyl PGD2

Target: GPR

16,16-dimethyl Prostaglandin D2

Cat.No: T36213

Synonym: 16,16-dimethyl Prostaglandin D2

Cat.No: T14211

Target: Others

Cat.No: T16280

Synonym: FPL 59002,尼多克罗

Target: Leukotriene Receptor, Prostaglandin Receptor, Histamine Receptor

Cat.No: T15712

Synonym: MK-0524

Target: Prostaglandin Receptor

Cat.No: T1866

Target: Others, PGE Synthase

Cat.No: T7652

Synonym: AM211 free acid

Target: Prostaglandin Receptor

Cat.No: T4624

Synonym: PGD2-inhibitor

Target: Prostaglandin Receptor

L 888607 Racemate

Cat.No: T15829

Target: Aurora Kinase

Cat.No: T41073

Cat.No: T10891

Synonym: Ramatroban analog

Target: P450

Cat.No: T38307

Cat.No: T21869

Cat.No: T38365

Prostaglandin J2

Cat.No: T73782

Cat.No: T38257

Cat.No: T71088

PROTAC(H-PGDS)-7

Cat.No: T41267

Cat.No: T35811

Cat.No: T38306

O-Desmethyl-N-deschlorobenzoyl Indomethacin

Cat.No: T36418

Cat. No.	Product Name	Target	Signaling Pathways
T13831	Prostaglandin D2 PGD2	Endogenous Metabolite	Metabolism
	Prostaglandin D2 (PGD2) (PGD2) 是哺乳动物大脑中主要产生的前列腺素之一，为最有效的内源性睡眠促进剂之一，并通过抑制炎症发挥保护作用。

天然产物

Prostaglandin D2

Cat.No: T13831

Synonym: PGD2

Target: Endogenous Metabolite

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