Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
T27084 |
Crisdesalazine
AAD2004,AAD 2004,AAD-2004 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Crisdesalazine (AAD 2004) 是微粒体前列腺素 E2 合酶 1 (mPGES-1) 的抑制剂。 Crisdesalazine 可减少自噬体形成、轴索病变和运动神经元变性,改善运动功能并延长寿命。 | |||
T38369 |
CAY10678
|
Prostaglandin Receptor; PD-1/PD-L1 | Apoptosis; Cell Cycle/Checkpoint; GPCR/G Protein; Immunology/Inflammation |
CAY10678 是一种 mPGES-1抑制剂,抑制 PD-1。CAY10678 可减少胶原沉积和T细胞耗竭,可用于研究黑色素瘤。 | |||
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。 | |||
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。 | |||
T16070 |
MF63
|
Others | Others |
MF63 is a selective mPGES-1 inhibitor (IC50: 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively). | |||
T25440 |
FR20
FR-20,FR 20 |
||
FR20 is a human microsomal prostaglandin synthase 1 (mPGES 1) inhibitor. | |||
T23862 |
CAY10589
CAY 10589,CAY-10589 |
||
CAY10589 is an mPGES-1 inhibitor. | |||
T12100 | mPGES1-IN-3 | Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
mPGES1-IN-3 is a potent and selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) . | |||
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... | |||
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. | |||
T63424 |
BRP-201
|
||
BRP-201 是一种选择性的、新型的、有效的 mPGES-1 抑制剂 (IC50: 0.42μM),被认为是下一代抗炎药治疗炎症性疾病的有希望的治疗靶点。 | |||
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。 | |||
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。 | |||
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。 |