Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T81181 | sEH/FLAP-IN-1 | FLAP | Immunology/Inflammation |
sEH/FLAP-IN-1(Compound 46A)是一sEH/FLAP抑制剂,具有阻断SACM刺激PBMC中5-LOX产物形成的活性(EC50: 11 nM),并能抑制sEH活性(EC50: 18 nM)及血栓素产生。该化合物适用于炎症性疾病研究领域。 | |||
T8844 |
Diflapolin
|
Others; FLAP; Epoxide Hydrolase | Immunology/Inflammation; Metabolism; Others |
Diflapolin 是高活性的双 5-脂氧合酶激活蛋白(FLAP)/可溶性环氧化物水解酶抑制剂,具有显著的抗炎作用和较高的靶向选择性。它抑制分离的 sEH 的活性,IC50为20 nM。它还抑制完整人单核细胞和中性粒细胞中 5-LOX 产物的形成,IC50分别为 30 和 170 nM。 | |||
T16087 |
Quiflapon
喹夫拉朋,MK-591 |
Apoptosis; FLAP | Apoptosis; Immunology/Inflammation |
Quiflapon (MK-591) 是一种选择性和特异性的FLAP 抑制剂,可诱导细胞凋亡。它也是口服白三烯生物合成抑制剂,在完整的人和诱导的大鼠多形核白细胞 PMNLs 中,其IC50值分别为 3.1 nM 和 6.1 nM。 | |||
T9023 |
Atuliflapon
AZD5718 |
FLAP | Immunology/Inflammation |
Atuliflapon (AZD5718) 是可口服的FLAP(5 -脂氧合酶激活蛋白)的抑制剂,IC50值为 2 nM,可用于冠状动脉疾病的研究。 | |||
T8545 |
FEN1-IN-4
FEN1 Inhibitor C2 |
Others | Others |
FEN1-IN-4 (FEN1 Inhibitor C2) 是人类皮瓣内切核酸酶-1 (hFEN1) 抑制剂。 | |||
T6893 |
MK-886
MK886,L 663536 |
Apoptosis; Leukotriene Receptor; COX; PPAR; FLAP | Apoptosis; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience |
MK-886 (L 663536)是一种细胞可渗透的,具有口服活性的 FLAP (IC50为 30 nM) 和白三烯生物合成 (完整白细胞和人全血中的IC50分别为 3 nM 和 1.1μM) 的抑制剂。它也是一种非竞争性PPARα拮抗剂,可以诱导细胞凋亡。 | |||
T11487 |
Fiboflapon
GSK2190915,AM-803 |
FLAP | Immunology/Inflammation |
Fiboflapon (GSK2190915) 是一种可口服且具有有效性 5-脂氧合酶激活蛋白 (FLAP) 抑制剂,结合 FLAP 的效价为 2.9 nM,对人血中 LTB4 有抑制作用, IC50 值为 76 nM。 | |||
T11487L |
Fiboflapon sodium
GSK2190915 sodium salt,AM-803 sodium |
LTR | Immunology/Inflammation |
Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood. | |||
TQ0098 |
Quiflapon sodium
喹夫拉朋钠,MK591 |
FLAP | Immunology/Inflammation |
Quiflapon sodium (MK591) is a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP). | |||
T13295 |
Veliflapon
DG-031,BAY X 1005 |
LTR | Immunology/Inflammation |
Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4. | |||
T77172 | Eflapegrastim | ||
Eflapegrastim 是一种人源化IgG4单抗 ,也是一种粒细胞集落刺激因子 (G-CSF)。Eflapegrastim 靶向G-CSF 受体 (c-Fms)。Eflapegrastim 刺激中性粒细胞祖细胞的增殖和分化,维持成熟和功能性中性粒细胞数目稳定。Eflapegrastim 还缩短中性粒细胞减少的持续时间。 | |||
T10314 |
AM103
AM 103 |
FLAP | Immunology/Inflammation |
AM103 是一种有效的特异性 FLAP 抑制剂 (IC50 = 4.2 nM)。 | |||
T9147 |
FEN1-IN-3
|
||
FEN1-IN-3 是一种人类皮瓣内切核酸酶-1 (hFEN1) 抑制剂,可使 hFEN1 稳定化,EC50为 6.8 μM。 | |||
T15274 |
FEN1-IN-1
LNT-1 |
Others | Others |
FEN1-IN-1 (LNT-1) 是一种FEN1的抑制剂,可绑定 FEN1 的活性位点,也可通过协调 Mg2+,进而表现出部分抑制作用。 | |||
T68449 |
JFD00950
|
||
JFD00950 is a human flap endonuclease 1 (FEN1) inhibitor with in vitro inhibition of flap cleavage activity as well as cytotoxic activity against a colon cancer cell line, DLD-1. | |||
T12793 |
(S)-BI 665915
|
Others | Others |
(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding).. | |||
T14205 |
AM679
|
Others | Others |
AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = | |||
T69418 |
AM-679
|
||
AM-679 is a 5-lipoxygenase-activating protein (FLAP) inhibitor. | |||
T69128 |
NSC-13755
|
||
NSC-13755 is a human flap endonuclease 1 (FEN1) inhibitor. | |||
T78192 |
FEN1-IN-5
|
FLAP | Immunology/Inflammation |
FEN1-IN-5(化合物12A),一种Flap内切酶1(FEN1,IC50=12 nM)的高效抑制剂,作用于DNA损伤修复过程。 | |||
T79389 |
LTB4-IN-2
|
FLAP | Immunology/Inflammation |
LTB4-IN-2(Compound 6x)是一种选择性的5-脂氧合酶激活蛋白(FLAP)抑制剂,旨在抑制白三烯B4(LTB4)的形成(IC50:1.15 μM),适用于抗炎研究。 | |||
T70316 |
AZD6642
|
||
AZD6642 is a potential and selective 5-Lipoxygenase activating Protein (FLAP) inhibitor. AZD6642 shows high specific potency and low lipophilicity resulting in a selective and metabolically stable profile. Based on initial PK/PD relations a low dose to human was predicted. | |||
T79134 |
FEN1-IN-6
|
FLAP | Immunology/Inflammation |
FEN1-IN-6(化合物9)是一种高效的Flap内切酶1(FEN1,IC50=10 nM)抑制剂,对哺乳动物细胞DNA损伤修复有关键作用。同时,FEN1-IN-6也针对相关酶,如XPG,表现出较强的抑制活性(IC50为23 nM)。 | |||
T40931 | FEN1-IN-2 | Others | Others |
FEN1-IN-2 是一种具有选择性和有效性的瓣内切酶 1 (FEN1) 的抑制剂,抑制 FEN1 和 XPG,具有潜在的抗癌活性,可用于研究DNA损伤修复。 | |||
T69970 |
AZD5718
|
||
AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease. | |||
T79135 |
FEN1-IN-7
|
FLAP | Immunology/Inflammation |
FEN1-IN-7(化合物16)是一款选择性Flap内切酶1(FEN1,IC50=18 nM)抑制剂,它在哺乳动物细胞的DNA损伤修复过程中发挥作用。此外,FEN1-IN-7对相关内切酶如着色性干皮病G蛋白(XPG,IC50=3.04 μM)也有靶向性。它能提高癌细胞对DNA烷基化剂或甲基化试剂的敏感性。 | |||
T37649 |
5(S),12(S)-DiHETE
|
||
5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotrie... |