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Search Results for " pgd2 "

36

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
T17232	Vidupiprant AMG 853	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Vidupiprant (AMG 853) 是一种有效的 CRTH2 和前列腺素 D 受体双重拮抗剂，在人源血浆中的 IC50 分别为 8 nM 和 35 nM。 Vidupiprant 可用于治疗哮喘的研究。
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。
T3520	Setipiprant KYTH-105,塞替匹仑,ACT-129968	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。
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。
T14565	BI-671800 AP-761,Cmpd A	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	BI-671800 (AP-761) 是高特异性的前列腺素 D2 受体拮抗剂，对哮喘有研究潜力，对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。
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。
T2690	Tranilast 曲尼司特,MK 341,SB 252218	RAAS; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	Tranilast (SB 252218) 是一种抗过敏药物，可抑制炎症细胞释放脂质介质和细胞因子，抑制前列腺素 D2 (PGD2)产生，IC50为 0.1 mM。它拮抗血管紧张素 II 并抑制其在血管平滑肌细胞中的生物学作用，具有抗炎和免疫调节作用。
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。
T2396	Ramatroban BAY u3405,雷马曲班	GPR; Prostaglandin Receptor; PPAR	DNA Damage/DNA Repair; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism
	Ramatroban (BAY u3405) 是一种血栓素 A(2) (TxA(2)) 拮抗剂，IC50为 14 nM。它还通过抑制PGD2结合从而拮抗CRTH2，IC50为113 nM。它用于治疗过敏性鼻炎，可用于治疗哮喘的研究。
T2664	Timapiprant OC000459	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	Timapiprant (OC000459) 是一种有效的选择性 D 前列腺素受体 2(DP2) 拮抗剂，IC50为 13 nM。它抑制肥大细胞激活 Th2 淋巴细胞和嗜酸性粒细胞，有效地置换来自人重组 DP2、大鼠重组 DP2 和人天然 DP2 的 [3H] PGD2。
T7359	CAY10471 Racemate TM30089 Racemate,3-[[(4-氟苯基)磺酰基]甲基氨基]-1,2,3,4-四氢-9H-咔唑-9-乙酸	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	CAY10471 Racemate (TM30089 Racemate) 是一种高选择性的 CRTH2/DP 2 受体拮抗剂，对 hCRTH2 的Ki 值为 0.6 nM，对其选择性远高于人血栓素 A2 受体 TP 或 PGD2 受体 DP。它对大小鼠的同源 CRTH2 也具有拮抗作用。
T13855	Quinotolast sodium FR71021	Others	Others
	Quinotolast sodium inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner in the concentration range of 1-100 μg/mL.
T69967	Laropiprant analog
	Laropiprant analog is an antagonist of the prostaglandin PGD2 receptor DP1.
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.
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).
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.
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.
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...
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...
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...
T15503	HQL-79	Others	Others
	HQL-79 is a selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor. It inhibits the synthesis of PGD2 and acts as an anti-allergic agent (Kd: 0.8 μM and IC50: 6 μM). It also shows no obvious effect on COX-1, COX-2, m-P
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。
T17099	Timapiprant sodium OC000459 sodium	Others	Others
	Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra
T38113	AL 6598
	Elevated intraocular pressure (IOP) is an important risk factor in developing glaucoma. Certain prostaglandins such as PGF2α and PGD2, have been shown to reduce IOP. AL 6598 is the isopropyl ester prodrug of AL 6556, a PGD2 receptor agonist that binds to DP receptors with a Ki value of 3.2 μM and demonstrates an EC50 value of 0.80 μM in an in vitro functional assay. Designed to enhance corneal absorption, AL 6598 produces a maximum 53% drop in IOP of the ocular hypertensive monkey with a 1 μg do...
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)。
T37506	MCTR2 MCTR2
	Maresin conjugates in tissue regeneration 2 (MCTR2) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages at the site of inflammation. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase then to MCTR2 by γ-glutamyl transferase. MCTR2 accelerates tissue regeneration in planaria (1 and 100 nM). Pretreatment with MCTR2 prior to E. coli administration reduces neutrophil infiltration, shor...
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...
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。
T37257	13,14-dihydro-15-keto Prostaglandin D1 13,14-dihydro-15-keto Prostaglandin D1
	Prostaglandin D1 (PGD1) is the theoretical D-series metabolite of dihomo-γ-linolenic acid (DGLA), but to date it has not been isolated as a natural product. It is an inhibitor of ADP-induced platelet aggregation in humans with an IC50 value of 320 ng/ml, about 1/10 as potent as PGD2. 13,14-dihydro-15-keto Prostaglandin D1 (13,14-dihydro-15-keto PGD1) is the theoretical metabolite of PGD1 via the 15-hydroxy PG dehydrogenase metabolic pathway. No biological studies for this compound have been repo...
T37300	PCTR1 PCTR1
	Protectin conjugates in tissue regeneration 1 (PCTR1) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid . DHA is oxidized to 16S,17S-epoxy-protectin, which is then converted to PCTR1 by glutathione S-transferase. PCTR1 levels increase during resolution of acute microbial-induced peritonitis in mice. PCTR1 (30 ng, i.p.) administration 12 hours post-infection increases macrophage numbers and activity and shortens the resolution phase of inflammation by 57%. It als...
T37275	2,3-dinor-11β-Prostaglandin F2α 2,3-dinor-11β-Prostaglandin F2α
	2,3-dinor-11β-Prostaglandin F2α (2,3-dinor-11β-PGF2α) was recovered from the urine of both normal monkeys and humans when infused with radiolabeled PGD2, where it represented approximately 1% and 4% of the infused radiolabeled dose, respectively. 2,3-dinor-11β-PGF2α has also been recovered from the urine of mastocytosis patients, where it is excreted in large amounts. In human asthmatic patients, 2,3-dinor-11β-PGF2α represents about 40% (as determined by GC/MS) of the immunoreactive 11β-PGF2α wh...
T37507	MCTR3 MCTR3
	Maresin conjugates in tissue regeneration 3 (MCTR3) is a specialized pro-resolving mediator (SPM) synthesized from docosahexaenoic acid in macrophages. DHA is oxidized to maresin 1 , which is converted to MCTR1 by glutathione S-transferase Mu 4 or leukotriene C4 synthase, then to MCTR2 by γ-glutamyl transferase, and to MCTR3 by dipeptidase. MCTR3 accelerates tissue regeneration in planaria (1 and 100 nM) approximately as potently as MCTR2 and more potently than MCTR1. Pretreatment with MCTR3 pri...
T23472	Tranilast Sodium	Others	Others
	Tranilast Sodium has been used for the treatment of bronchial asthma. Tranilast is also used to autoimmune diseases, atopic and fibrotic pat.

化合物

Cat.No: T4624

Synonym: PGD2-inhibitor

Target: Prostaglandin Receptor

HPGDS inhibitor 1

Cat.No: T1804

Synonym: HPGDS-inhibitor-1

Target: PGE Synthase

Cat.No: T17232

Synonym: AMG 853

Target: Prostaglandin Receptor

15(R)-15-methyl Prostaglandin D2

Cat.No: T37264

Synonym: 15(R)15methyl PGD2

Target: GPR

Cat.No: T3520

Synonym: KYTH-105,塞替匹仑,ACT-129968

Target: GPR, Prostaglandin Receptor

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: T14565

Synonym: AP-761,Cmpd A

Target: GPR, Prostaglandin Receptor

Cat.No: T7652

Synonym: AM211 free acid

Target: Prostaglandin Receptor

Cat.No: T2690

Synonym: 曲尼司特,MK 341,SB 252218

Target: RAAS, Prostaglandin Receptor

Cat.No: T1866

Target: Others, PGE Synthase

Cat.No: T2396

Synonym: BAY u3405,雷马曲班

Target: GPR, Prostaglandin Receptor, PPAR

Cat.No: T2664

Synonym: OC000459

Target: GPR, Prostaglandin Receptor

CAY10471 Racemate

Cat.No: T7359

Synonym: TM30089 Racemate,3-[[(4-氟苯基)磺酰基]甲基氨基]-1,2,3,4-四氢-9H-咔唑-9-乙酸

Target: GPR, Prostaglandin Receptor

Quinotolast sodium

Cat.No: T13855

Synonym: FR71021

Target: Others

Laropiprant analog

Cat.No: T69967

Cat.No: T38257

15(S)-15-methyl Prostaglandin D2

Cat.No: T36153

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

Prostaglandin D2 methyl ester

Cat.No: T36545

Synonym: Prostaglandin D2 methyl ester

16,16-dimethyl Prostaglandin D2

Cat.No: T36213

Synonym: 16,16-dimethyl Prostaglandin D2

Cat.No: T38365

tetranor-PGDM

Cat.No: T38306

Prostaglandin D2 Ethanolamide

Cat.No: T38389

Synonym: Prostaglandin D2 Ethanolamide

Cat.No: T15503

Target: Others

Cat.No: T21869

Timapiprant sodium

Cat.No: T17099

Synonym: OC000459 sodium

Target: Others

Cat.No: T38113

Prostaglandin J2

Cat.No: T73782

Cat.No: T37506

Synonym: MCTR2

Cat.No: T35811

PROTAC(H-PGDS)-7

Cat.No: T41267

13,14-dihydro-15-keto Prostaglandin D1

Cat.No: T37257

Synonym: 13,14-dihydro-15-keto Prostaglandin D1

Cat.No: T37300

Synonym: PCTR1

2,3-dinor-11β-Prostaglandin F2α

Cat.No: T37275

Synonym: 2,3-dinor-11β-Prostaglandin F2α

Cat.No: T37507

Synonym: MCTR3

Tranilast Sodium

Cat.No: T23472

Target: Others

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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