Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10410 |
ATX inhibitor 1
|
PDE | Metabolism |
ATX inhibitor 1是一种 ATX(IC50=1.23 nM, FS-3; 2.18 nM, bis-pNPP) 抑制剂。 | |||
T10409 |
ATX inhibitor 5
|
PDE | Metabolism |
ATX inhibitor 5 是一种有效且具有口服活性的 autotaxin (ATX) 抑制剂(IC50 : 15.3 nM),可降低 CCl4 诱导的肝纤维化水平,具有抗肝纤维化作用,。 | |||
T39190 | ATX-002 | ||
ATX-002 is a property-tunable lipid for RNA drug delivery. | |||
T39136 |
ATX inhibitor 7
|
||
ATX inhibitor 7 is a autotaxin inhibitor and shows good oral exposure. | |||
T80039 |
ATX-II
|
Sodium Channel | Membrane transporter/Ion channel |
ATX-II为特定Na+通道调节剂,源自海葵(Anemonia sulcata)毒液。该化合物会使细胞培养物对Na+Halothane、Caffeine及Ryanodine敏感,并可诱发肺静脉心律失常及心房颤动。 | |||
T27324 |
FK614
FK 614,ATx-08-001,ATx-08001,FK-614 |
||
FK-614 is a selective agonist of peroxisome proliferator-activated receptor gamma. FK-614 improves peripheral glucose utilization while decreases hepatic insulin extraction in alloxan-induced diabetic dogs. | |||
T64141 |
ATX inhibitor 11
|
||
ATX inhibitor 11 是 ATX (autotaxin) 的有效抑制剂 (IC50: 2.7 nM)。ATX inhibitor 11 能够缓解小鼠纤维化模型中纤维化组织的严重程度,有效减少纤维化生物标志物 α-SMA 的沉积。ATX inhibitor 11 能够用于研究肺纤维化。 | |||
T64210 |
ATX inhibitor 13
|
||
ATX inhibitor 13 (compound 10c) 是一种口服具有活力的 ATX 抑制剂 (IC50: 3.4 nM)。ATX inhibitor 13 能够将RAW264.7 细胞的细胞周期阻滞在 G2 期,抑制细胞的增殖和迁移,诱导细胞凋亡。ATX inhibitor 13 对肿瘤细胞集落形成表现出抑制作用。 | |||
T63325 |
ATX inhibitor 9
|
||
ATX inhibitor 9 是增稠的杂芳基衍生物化合物,也是 ATX 的有效抑制剂。其中 Autotaxin (ATX),也称为 ENPP2,是一种主要在肺癌细胞、支气管上皮细胞和肺泡巨噬细胞中高度表达的分泌酶。ATX inhibitor 9 对癌症或纤维退行性疾病具有研究潜力。 | |||
T63904 |
ATX inhibitor 19
|
||
ATX inhibitor 19 是 ATX 的有效抑制剂 (IC50: 156 nM)。 | |||
T63564 | ATX inhibitor 22 | ||
ATX inhibitor 22 是 ATX (autotaxin) 的新型抑制剂 (IC50: 218.9 μM),对 LPAR1 缺乏抑制活性。 | |||
T63584 | ATX inhibitor 12 | ||
ATX inhibitor 12 是口服具有活力的 ATX 抑制剂 (IC50: 1.72 nM)。在 C57Bl/6J 小鼠中,口服剂量为 60 mg/kg 的 ATX inhibitor 12 时,能够有效抑制肺结构损伤,降低纤维化病变。ATX inhibitor 12 能够用于研究特发性肺纤维化 (IPF) 。 | |||
T63845 |
ATX inhibitor 14
|
||
ATX inhibitor 14 是基于吲哚的氨基甲酸酯衍生物,是一种自粘蛋白 (ATX) 的有效抑制剂 (IC50: 0.41 nM),对纤维化相关疾病表现出研究潜力。 | |||
T63524 |
ATX inhibitor 10
|
||
ATX inhibitor 10 是一种含氮杂环化合物,是一种 ATX 的有效抑制剂。其中 ATX 在引起包括纤维化、神经变性、关节炎、神经性疼痛和癌症在内的病理中发挥作用。ATX inhibitor 10 对 ATX 相关疾病表现出研究潜力。 | |||
T64130 |
ATX inhibitor 16
|
||
ATX inhibitor 16 是一种 ATX 的有效抑制剂 (IC50: 0.0021 μM)。ATX inhibitor 16 对乳腺癌细胞表现出明显的抗增殖作用。 | |||
T72681 | ATX inhibitor 17 | ||
ATX inhibitor 17 是一种有效的ATX 抑制剂,IC50为 0.019 µM。 ATX inhibitor 17 在乳腺癌细胞中显示出优异的抗增殖活性。 | |||
T82936 |
ATX-II TFA
|
Sodium Channel | Membrane transporter/Ion channel |
ATX-II TFA为源自海葵(Anemonia sulcata)毒素的特定Na+通道调节剂,能使细胞培养物对Na+、Halothane、Caffeine和Ryanodine敏感,并可诱发肺静脉心律失常和心房颤动。 | |||
T63510 |
ATX inhibitor 21
|
||
ATX inhibitor 21 是 ATX 的有效抑制剂 (IC50: 3490 nM)。 | |||
T63829 |
ATX inhibitor 20
|
||
ATX inhibitor 20 是 ATX 的有效抑制剂 (IC50: 2.3 nM)。 | |||
T63612 | ATX inhibitor 8 | ||
ATX inhibitor 8 是自分泌运动因子 Autotaxin (ATX) 抑制剂。 | |||
T61612 |
ATX inhibitor 15
|
||
ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. Additionally, ATX inhibitor 15 effectively inhibits ATX activity in vivo and suppresses the expression of pro-fibrotic genes. Furthermore, ATX inhibitor 15 exhibits protective effects in lung fibrosis induced by Bleomycin in mice [1]. | |||
T31101 |
CRT0273750
CRT 0273750,CRT-0273750 |
PDE | Metabolism |
CRT0273750 是一种 ATX 抑制剂的先导化合物,可调节血浆中 LPA 水平,用于 ATX/LPA 依赖性癌症模型。 | |||
T11533 |
Z-HA155
CS-963 |
PDE | Metabolism |
Z-HA155 (CS-963) 是一种高效的 ATX 选择性抑制剂,其 IC50=5.7 nM。 | |||
TP2027 |
GaTx2
|
||
Very high affinity ClC-2 blocker (apparent KD ~ 50 pM). Slows ClC-2 activation and inhibits slow-gating but does not inhibit open ClC-2 channels. Selective for ClC-2 over other ClC family members (ClC-0, ClC-1, ClC-3 and ClC-4), CFTR, GABAC, CaCC and KV1. | |||
T38759 |
ONO-8430506
|
PDE | Metabolism |
ONO-8430506 是一种可口服的、具有有效性的 autotaxin (ATX)/ENPP2 抑制剂( IC90 :100 nM),能够抑制小鼠血浆中 ATX 活性。 | |||
T22086 |
HA 155
Autotaxin Inhibitor IV |
PDE | Metabolism |
HA 155 (Autotaxin Inhibitor IV) 是一种基于硼酸的化合物,通过选择性结合其催化苏氨酸来抑制 ATX,IC50 为 5.7 nM。 | |||
T2646 |
HA130
|
PDE | Metabolism |
HA130 是选择性 autotaxin 抑制剂,IC50=28 nM。 | |||
T10545 |
BIO-32546
|
PDE | Metabolism |
BIO-32546 (S-isomer) 是一种高效的 autotaxin (ATX) 的调节剂,IC50 值为 1 nM。 | |||
T4041 |
Ziritaxestat
GLPG1690 |
PDE | Metabolism |
Ziritaxestat (GLPG1690) 是一种创新的 autotaxin (ATX)抑制剂,其 IC50=131 nM,Ki=15 nM。 | |||
T10415 |
Autotaxin-IN-3
|
PDE | Metabolism |
Autotaxin-IN-3 是 Autotaxin 的抑制剂(IC50 = 2.4 nM),Autotaxin 负责增加腹水和血浆中的溶血磷脂酸。 | |||
T14560 | BI-2545 | Others | Others |
BI-2545 is an autotaxin (ATX) inhibitor that significantly reduces LPA. For human ATX and rat ATX, the IC50s values are 2.2 nM and 3.4 nM , respectively. | |||
T3631 |
PF-8380
|
PDE | Metabolism |
PF8380 是有效的autotaxin 抑制剂,在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。 | |||
T72837 | Autotaxin-IN-6 | ||
Autotaxin-IN-6 (compound 23),一种ATX (自分泌运动分子)抑制剂,具有30 nM的IC50值,能够减少细胞迁移,适用于抗癌研究。 | |||
T27433 |
GRI918013
GRI 918013,GRI-918013 |
||
GRI918013 is an ATX inhibitor. | |||
T81804 | MEY-003 | ||
MEY-003是针对Autotaxin(ATX)的抑制剂,具有对hATX-β和hATX-ɣ的EC50值分别为460 nM和1.09 μM(LPC18:1分析条件下)。作为一种非竞争性抑制剂,其Ki值为432 nM。该化合物主要应用于ATX相关疾病的研究领域。 | |||
T70275 |
PAT-347
|
||
PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others. | |||
T28300 |
PAT-347 sodium
PAT-347,PAT347,PAT 347 |
||
PAT-347 is a potent inhibitor of Autotaxin (ATX), a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. | |||
T69652 |
Relutrigine
PRAX-562 |
||
Relutrigine (PRAX-562) 是一种口服活性的持久性钠通道 (sodium channel) 抑制剂,能够有效优先抑制由 ATX-II (Nav 1.5 激活剂) 或 SCN8A 突变 N1768D 引起的持续性 INa,其 IC50 值分别为 141 nM 和 75 nM。该化合物通过使用依赖性阻断方式,降低神经元的内在兴奋性,显示出明显的抗惊厥活性。 | |||
T16434 |
PAT-048
|
PDE | Metabolism |
PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. | |||
T38488 |
S32826
|
||
S32826 is a highly potent inhibitor of autotaxin, exhibiting an IC50 value of 8.8 nM. It displays comparable inhibitory properties towards various autotaxin isoforms, including α, β, and γ. Furthermore, S32826 effectively inhibits the release of LPA from adipocytes. | |||
T23293 |
S32826 disodium
S 32826 |
Others | Others |
autotaxin inhibitor | |||
T14352 |
Autotaxin-IN-1
|
PDE | Metabolism |
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship and it is used in treatment of osteoarthritis pain[1]. |