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26

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
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。
T37778 19(R)-hydroxy Prostaglandin E1

19(R)-hydroxy Prostaglandin E1

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

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。
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。
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。
T36726 6-keto Prostaglandin E1

6-keto Prostaglandin E1

6-keto Prostaglandin E1 是 PGE1 的生物活性衍生物,在抗血小板聚集和解聚作用方面发挥作用。
T36770 11-deoxy Prostaglandin E1

11-deoxy Prostaglandin E1

11-deoxy Prostaglandin E1 是前列腺素 E1类似物,具有支气管扩张活性,可抑制组胺诱导的支气管收缩,引起离体豚鼠的气管条松弛。
T36159 8-iso Prostaglandin E1

8-iso Prostaglandin E1

8-iso Prostaglandin E1 能引起犬肺静脉中的痉挛,还能够起到血管舒张作用。
T36775 13,14-dihydro Prostaglandin E1

13,14-dihydro Prostaglandin E1

13,14-dihydro Prostaglandin E1 (13,14-dihydro PGE1) is a biologically active metabolite of PGE1 with comparable potency to the parent compound. It is an inhibitor of ADP-induced platelet aggregation in human PRP and washed platelets with IC50 values of 31 and 21 nM, respectively. 13,14-dihydro PGE1 is a slightly more potent inhibitor of ADP-induced human platelet aggregation than PGE1 which has an IC50 value of 40 nM. Also, 13,14-dihydro PGE1 was shown to activate adenylate cyclase in NCB-20 hyb...
T36214 16,16-dimethyl Prostaglandin E1

16,16-dimethyl Prostaglandin E1

16,16-dimethyl Prostaglandin E1 是 PGE1 (T1626) 类似物,可诱导支气管收缩和血管平滑肌收缩,并抑制吲哚美辛诱导的细胞伸长。
T36219 1a,1b-dihomo Prostaglandin E1

1a,1b-dihomo Prostaglandin E1

1a,1b-dihomo Prostaglandin E1 是一类前列腺素化合物。
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.
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

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

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

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

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

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

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

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

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...

化合物

hPGDS-IN-1
Cat.No: T2681
Synonym:
Target: PGE Synthase
19(R)-hydroxy Prostaglandin E1
Cat.No: T37778
Synonym: 19(R)-hydroxy Prostaglandin E1
Target:
13,14-dihydro-15-keto Prostaglandin E1
Cat.No: T36147
Synonym: 13,14-dihydro-15-keto Prostaglandin E1
Target:
HPGDS inhibitor 1
Cat.No: T1804
Synonym: HPGDS-inhibitor-1
Target: PGE Synthase
PGS-IN-1
Cat.No: T10098
Synonym: KME-4
Target: Lipoxygenase, Prostaglandin Receptor
CAY10526
Cat.No: T23861
Synonym: CAY-10526,BTH,CAY 10526
Target: Prostaglandin Receptor
6-keto Prostaglandin E1
Cat.No: T36726
Synonym: 6-keto Prostaglandin E1
Target:
11-deoxy Prostaglandin E1
Cat.No: T36770
Synonym: 11-deoxy Prostaglandin E1
Target:
8-iso Prostaglandin E1
Cat.No: T36159
Synonym: 8-iso Prostaglandin E1
Target:
13,14-dihydro Prostaglandin E1
Cat.No: T36775
Synonym: 13,14-dihydro Prostaglandin E1
Target:
16,16-dimethyl Prostaglandin E1
Cat.No: T36214
Synonym: 16,16-dimethyl Prostaglandin E1
Target:
1a,1b-dihomo Prostaglandin E1
Cat.No: T36219
Synonym: 1a,1b-dihomo Prostaglandin E1
Target:
1a,1b-dihomo Prostaglandin E2
Cat.No: T36045
Synonym: 1a,1b-dihomo Prostaglandin E2
Target:
Limaprost
Cat.No: T15757
Synonym: 17α,20-dimethyl-δ2-PGE1,利马前列素,OP1206,ONO1206
Target: PGE Synthase
mPGES-1 Inhibitor-1
Cat.No: T28089
Synonym:
Target: Prostaglandin Receptor
PF-9184
Cat.No: T21738
Synonym:
Target: Prostaglandin Receptor
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
Friluglanstat
Cat.No: T79846
Synonym:
Target: PGE Synthase
Zaloglanstat
Cat.No: T39000
Synonym: GRC-27864,ISC-27864
Target:
PF-4693627
Cat.No: T16504
Synonym:
Target: Prostaglandin Receptor
8(E),10(E),12(Z)-Octadecatrienoic Acid
Cat.No: T36887
Synonym:
Target:
UT-11
Cat.No: T74781
Synonym:
Target:
Butaprost
Cat.No: T26925
Synonym: Butaprostum,TR-4979,(R)-Butaprost
Target:
AF3442
Cat.No: T68334
Synonym:
Target:
Prostaglandin E2 Inhibitor 3
Cat.No: T83773
Synonym: PGE2 Inhibitor 3
Target:
Prostaglandin Bx
Cat.No: T35961
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
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。

天然产物

Prostaglandin E1
Cat.No: T1626
Synonym: 前列地尔,PGE1,列腺素E1,Alprostadil
Target: Endogenous Metabolite, Prostaglandin Receptor
Tussilagone
Cat.No: T6S1027
Synonym:
Target: Others
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