Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T73611 | Kallikrein | ||
Kallikrein 能够在血浆和组织中形成激肽释放酶激肽系统(KKS),分别产生缓激肽和激肽肽。 | |||
T40312 | Plasma kallikrein-IN-1 | ||
Plasma kallikrein-IN-1 is a PKK inhibitor with an IC 50 value of 0.5 nM. | |||
T63579 |
Kallikrein-IN-1
|
||
Kallikrein-IN-1 (Formula A) 是一种激肽释放酶 Kallikrein 抑制剂。 | |||
T63796 |
Kallikrein-IN-2
|
||
Kallikrein-IN-2 (compound 1) 是一种激肽释放酶 Kallikrein 的抑制剂。 | |||
T72337 | Plasma kallikrein-IN-2 | ||
Plasma kallikrein-IN-2 是一个有效的 plasma kallikrein (PKal)抑制剂,IC50值为 0.1 nM。Plasma kallikrein-IN-2 可用于遗传性血管水肿、糖尿病性黄斑水肿、糖尿病视网膜病变的研究。 | |||
T72624 |
Kallikrein 5-IN-2
|
||
Kallikrein 5-IN-2 是一种选择性 KallikreinKLK5抑制剂 (pIC50=7.1)。KLK5 抑制可以使表皮脱落正常化并减少相关的炎症和瘙痒。 | |||
T61403 |
Plasma kallikrein-IN-3
|
||
Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1]. | |||
T11885 |
LSP-249
|
Others | Others |
LSP-249是血浆 kallikrein 的抑制剂,用于血管性水肿的研究,EC50值小于 100 nM。 | |||
T14358 |
Avoralstat
BCX4161 |
Others | Others |
Avoralstat (BCX4161) 是血浆激肽释放酶(PKK)抑制剂,具有口服活性,可用于遗传性血管性水肿的研究。 | |||
T3359 |
Aprotinin
抑酶肽,抑肽酶,Bovine Pancreatic Trypsin Inhibitor,Traskolan,Antilysin |
Others; Serine Protease; Influenza Virus; Proteasome | Microbiology/Virology; Others; Proteases/Proteasome; Ubiquitination |
Aprotinin (Traskolan) 是分离自牛肺的一种广谱丝氨酸蛋白酶抑制剂,可抑制多种不同酯酶和蛋白酶的活性。 | |||
T6370 |
AEBSF hydrochloride
AEBSF HCl,Pefabloc SC |
Thrombin; Serine Protease; Influenza Virus | Microbiology/Virology; Proteases/Proteasome |
AEBSF hydrochloride (Pefabloc SC) 是一种丝氨酸蛋白酶的不可逆抑制剂。 | |||
T39350 |
Sebetralstat
KVD900 |
Others | Others |
Sebetralstat (KVD900) 是一种血浆激肽释放酶抑制剂,可用于代谢性疾病的研究。 | |||
TP1792L |
KKI-5 acetate(97145-43-2 free base)
|
Serine Protease | Proteases/Proteasome |
KKI-5 acetate(97145-43-2 free base) 是一种丝氨酸蛋白酶抑制剂,可抑制激肽释放酶和纤溶酶。 KKI 5 可能表现出抗癌化疗益处,也可用作血管性水肿的治疗方法。 | |||
T68173 |
ZD-2138
Ici-D2138 |
Lipoxygenase | Metabolism |
ZD-2138是一种有效且具有选择性的5-脂氧合酶(5-LOX)的特异性抑制剂,抑制了过敏原诱导的肺支气管收缩,可减少豚鼠孤立气道的神经诱发性快速激肽能收缩。ZD-2138可用来治疗哮喘疾病。 | |||
T0372 |
Gabexate mesylate
甲磺酸加贝酯,FOY |
Factor Xa; Serine Protease; Proteasome | Metabolism; Proteases/Proteasome; Ubiquitination |
Gabexate mesylate (FOY) 是一种非抗原的类胰蛋白酶丝氨酸蛋白酶抑制剂。 | |||
T21610 |
Bradykinin (acetate)
|
Bradykinin Receptor | GPCR/G Protein |
Bradykinin (acetate) 是一种由激肽释放酶-激肽系统产生的活性肽。它是一种炎症介质,也被认为是多种血管和肾功能的神经介质和调节剂。它由血液中的 kallidin 酶促产生,是一种强大的血管扩张剂,可引起平滑肌收缩,并可能介导炎症。它具有作为人血清代谢物和血管扩张剂的作用。它是缓激肽 (2+) 的互变异构体。 | |||
T70161 |
Berotralstat HCl
|
||
Berotralstat HCl is a novel selective inhibitor of plasma kallikrein, blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE. | |||
T37033 |
H-D-Pro-Phe-Arg-pNA . 2 HCl
|
||
pFR-pNA, chromogenic substrate for the determination of plasma kallikrein-like activity. CAS Number (net): 64816-19-9. | |||
T82510 |
Ecallantide TFA
DX-88 TFA |
||
Ecallantide (DX-88) TFA 是一种特异性的重组血浆激肽释放酶(Kallikrein)抑制剂,作用于缓激肽的生成过程以减少其产生。此化合物主要用于预防和治疗血管性水肿的急性攻击。 | |||
T71417 |
LM-030
|
||
LM-030, also known as BPR277, is a novel inhibitor of kallikrein-related peptidase 7 (KLK7) and epidermal elastase 2 (ELA2). | |||
T80271 |
Irucalantide
|
||
Irucalantide 是一种激肽释放酶(kallikrein)抑制剂,能够阻碍这种酶的活性,从而影响相关的生物过程。 | |||
T35579 |
PKSI-527
|
||
PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of in... | |||
T77999 |
KKI-5 TFA
|
||
KKI-5 (TFA)为特异性组织激肽释放酶抑制剂,能有效减少乳腺癌细胞的浸润性。 | |||
T63507 |
Feniralstat
|
||
Feniralstat 是吡唑衍生物,是一种激肽释放酶 (kallikrein) 的有效抑制剂,能够抑制人血浆激肽释放酶 (pKal) (IC50: 6.7 nM)。Feniralstat 不抑制人 KLK1、人 FXIa 和人因子 Xlla (IC50均 >40 μM)。 | |||
TP1379 |
KKI-5 TFA(97145-43-2 free base)
KKI-5 (TFA) |
||
KKI-5 (TFA) is a specific tissue kallikrein inhibitor.Kki-5 (TFA) can reduce breast cancer cell infiltration. | |||
T35869 |
Berotralstat
|
||
Berotralstat (BCX7353) is a second-generation, synthetic, and orally active plasma kallikrein inhibitor with low toxicity. It is highly specific and effectively used in the research of hereditary angioedema (HAE) attacks. Berotralstat functions by inhibiting the enzymatic activity of plasma kallikrein, which is responsible for the release of bradykinin. This blocking mechanism targets the major biologic peptide involved in the promotion of swelling and pain associated with HAE attacks[1][2]. | |||
TP1013 |
N-CBZ-Phe-Arg-AMC
Z-FR-AMC |
||
N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a substrate for serine proteases, including cathepsins, kallikrein and plasmin. Absorption/emission of substrate = 330/390 nm (weak fluorescence); absorption/emission of end product (AMC) = 342/441 nm (strong fluorescence). | |||
T80095 |
D-Pro-Phe-Arg-Chloromethylketone
|
Factor Xa | Metabolism |
D-Pro-Phe-Arg-Chloromethylketone是一种抑制剂,它针对凝血因子XII (coagulation factor XII) 和血浆激肽释放酶 (kallikrein),在血栓形成和炎症过程中具有关键作用。 | |||
T69777 |
DKFZ-251
|
||
DKFZ-251 is a potent inhibitor of kallikrein-related peptidase 6 with on-target cellular activity. DKFZ-251 demonstrated good selectivity for KLK6 compared to other KLKs, and on-target activity in a cellular assay. | |||
T78572 |
Ecallantide
DX-88 |
||
Ecallantide (DX-88) 是高特异性重组血浆激肽释放酶抑制剂,用于阻断缓激肽生成,治疗血管性水肿急性发作。 | |||
TP1792 |
KKI-5
|
||
KKI 5 is a serine protease inhibitor that inhibits kallikrein and plasmin. KKI 5 may exhibit anticancer chemotherapeutic benefit and may also be used as a treatment for angioedema. | |||
T6564L |
Leupeptin
Leupeptin Ac-LL,NK-381 |
||
Leupeptin is a competitive protease inhibitor produced by actinomycetes. Leupeptin can inhibit cysteine, serine and threonine peptidases. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine p | |||
T69297 |
Leupeptin HCl
|
||
Leupeptin is a naturally occurring protease inhibitor that can inhibit cysteine, serine and threonine peptidases. Leupeptin is an organic compound produced by actinomycetes. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine proteinases (papain, cathepsin B (Ki = 4.1 nM), endoproteinase Lys-C). It does not inhibit α-chymotrypsin or thrombin. Leupeptin is a competitive transition state inhibitor and its inhibition may be relieved by... | |||
T76248 |
Tutuilamide A
|
||
Tutuilamide A为一有效抑制剂,针对猪胰弹性蛋白酶(PPE)展现出1.2 nM的IC50值。此外,该化合物亦对人中性粒细胞弹性蛋白酶(HNE; IC50=0.73 nM)及激肽释放酶7(KLK7; IC50=5.0 nM)有抑制作用。 | |||
T76710 |
Lanadelumab
|
||
Lanadelumab (SHP643) 是一种针对血浆激肽释放酶 (plasma kallikrein (pKal)) 的人源化IgG1单克隆抗体,Ki 值为 0.12 nM。Lanadelumab 抑制游离和 HMWK 结合的 pKal。Lanadelumab 具有研究遗传性血管性水肿的潜力 | |||
T70170 |
Milvexian TFA
|
||
Milvexian, also known as BMS-986177 and JNJ-70033093, is a blood coagulation factor XIa inhibitor. Milvexian demonstrated good selectivity over plasma kallikreinKi = 44 nM (400-fold selective), and chymotrypsinKi = 35 nM (318-fold selective). At a dose of 1.5 mg/kg, Milvexian exhibited an overall exposure of 1215 nM/h, low clearance of 10.3 mL/min/kg, and oral bioavailability of 32%. |