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43

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T78018 Plasminogen

Plasminogen是一种可由尿激酶血浆蛋白原激活剂(uPA)或组织血浆蛋白原激活剂(tPA)裂解激活的分泌性蛋白,生成血浆蛋白,该酶可以广泛裂解纤维蛋白及其他ECM成分。作为促炎调节剂,Plasminogen能促进急性及糖尿病相关伤口愈合。该蛋白在伤口愈合、炎症和低纤溶酶原血症的研究中有重要应用。
T13408 ZK824190

Others; Serine Protease Others; Proteases/Proteasome
ZK824190 是具有口服活性尿激酶型纤溶酶原激活剂 (uPA) 选择性抑制剂,对 uPA,tPA 和 Plasmin 的IC50分别为 237,1600 和 1850 nM。ZK824190在多发性硬化症中有研究价值。
T28788 SK-216

SK216.Plasminogen activator inhibitor-1 (PAI-1) inhibitor

SK-216 is a specific PAI-1 inhibitor. SK-216 reduced the extent of angiogenesis in the tumors and inhibited VEGF-induced migration and tube formation by human umbilical vein endothelial cells in vitro. SK-216 reduced the degree of bleomycin-induced pulmon
T8962 TM5007

PAI-1 Metabolism
TM5007 是纤溶酶原激活物抑制剂-1(PAI-1;IC50 为 29 uM)的强效抑制剂。
T4254 TM5441

PAI-1; Apoptosis Apoptosis; Metabolism
TM5441 是口服生物可利用的纤溶酶原激活物抑制剂-1 抑制剂,抑制多个癌症细胞系的 IC50值在 13.9 到 51.1 μM。它诱导几种人类癌症细胞的内在调亡,减弱 Nω-硝基-1-精氨酸甲酯诱导的心脏高血压和血管衰老。
T3442 UK-371804

UK371804

PAI-1; Serine Protease Metabolism; Proteases/Proteasome
UK-371804 是一种尿嘧啶型纤溶酶原激活物的抑制剂,Ki=10 nM。
T13257 Upamostat

PAI-1; Serine/threonin kinase; Serine Protease Cell Cycle/Checkpoint; Metabolism; Proteases/Proteasome
Upamostat 是一种丝氨酸蛋白酶抑制剂,也是一种具有口服活性的 WX-UK1 前药,是一种尿激酶型纤溶酶原激活剂 (uPA) 抑制剂。
T4255 TM5275 sodium

TM5275 sodium salt

PAI-1 Metabolism
TM5275 sodium (TM5275 sodium salt) 是一种纤溶酶原激活物抑制剂,IC50=6.95 μM。
T2030 Tiplaxtinin

PAI-039,Tiplasinin

PAI-1; Apoptosis Apoptosis; Metabolism
Tiplaxtinin (Tiplasinin) 是一种具有口服活性的选择性纤溶酶原激活物抑制剂-1 抑制剂,IC50为 2.7 μM。
T29856 Aleplasinin

PAZ 417,PAZ417,PAZ-417

PAI-1 Metabolism
Aleplasinin (PAZ 417) 是纤溶酶原激活物抑制剂 1 (PAI-1) 的选择性和口服活性抑制剂,是纤溶系统的关键负调节剂。 Aleplasinin 可用于阿尔茨海默病研究。
T8362 Benzamidine hydrochloride

Benzamidine HCl,苄脒盐酸盐

Serine/threonin kinase; Serine Protease Cell Cycle/Checkpoint; Metabolism; Proteases/Proteasome
Benzamidine hydrochloride (Benzamidine HCl) 是可逆的胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 竞争性抑制剂,对 uPA、类胰蛋白酶、胰蛋白酶和 Xa 因子作用的Ki 分别为 97 µM、20 µM、21 µM 和 110 µM。
TP2338L Cenupatide acetate

Cenupatide acetate(1006388-38-0 Free base)

Others Others
Cenupatide acetate 是一种尿激酶纤溶酶原激活物受体 (uPAR) 抑制剂,用于治疗与细胞迁移改变相关的疾病,例如癌症。
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。
T60248 4-Aminobenzamidine dihydrochloride

p-Aminobenzamidine dihydrochloride

Serine Protease Proteases/Proteasome
4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) 是一种强胰蛋白酶 (trypsin)抑制剂,也是一种相对较弱的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂 (Ki=82 μM)。4-Aminobenzamidine 可抑制 SCID 小鼠体内前列腺肿瘤的生长。
T71851 5-trans-Prostaglandin E2

5-trans-Prostaglandin E2 accelerates fibrinolysis by enhancing plasminogen activation mediated by tissue-type plasminogen activator. It also inhibits platelet aggregation in human PRP.
T13251 UKI-1

UKI-1C

Others Others
UKI-1 is a urokinase-type plasminogen activator system synthetic inhibitor.
T70734 U46,195

U46,195 stimulates the production of tissue-type plasminogen activator, and is a PAF antagonist.
T70417 XR 1853

XR 1853 is a low molecular weight modulator of human plasminogen activator inhibitor-1 activity.
T69751 UK-356202

UK-356,202 is a potent and selective urokinase-type plasminogen activator (Ki = 37 nM). Urokinase plasminogen activator (uPA, urokinase) is a trypsinlike serine protease and a therapeutical target for many cancer types, including breast, ovarian, and pancreatic cancer. uPA is a valuable oncology target.
T68572 IMD-1622

IMD-1622 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor.
T69890 PS-519

PS-519 is a human tissue plasminogen activator and proteasome inhibitor.
T68659 Valyl-glycyl-arginine-4-nitroanilide

Valyl-glycyl-arginine-4-nitroanilide is a tissue plasminogen activator.
T69319 U 34599

U 34599 stimulates the production of tissue-type plasminogen activator.
T25915 Diaplasinin

PAI-749,PAI749,PAI 749

PAI-749 is a selective and effective antagonist agent of plasminogen activator inhibitor 1 (PAI-1).
T13409L ZK824859 hydrochloride (2271122-53-1 free base)

ZK824859 hydrochloride

Others Others
ZK824859 hydrochloride is an oral available and selective inhibitor of urokinase plasminogen activator (uPA)(IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively).
T70927 UCD74A HCl

UCD74A HCl is a cell impermeant homolog of UCD38B, inhibitor of uPA (urokinase plasminogen activator).
T13409 ZK824859

Others Others
ZK824859 is an oral available and selective inhibitor of urokinase plasminogen activator (uPA)(IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively).
T41085 UK122

UK122

UK122 is a highly effective and specific inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 value of 0.2 μM. It displays negligible to minimal inhibition towards tissue-type plasminogen activator (tPA), plasmin, thrombin, and trypsin (all IC50 >100 μM). Functioning as a 4-oxazolidinone analogue, UK122 is an anticancer agent that effectively inhibits cancer cell migration and invasion.
T70810 THR-18

THR-18 is an 18-mer peptide derived from the sequence of human plasminogen activator inhibitor 1 (PAI-1), having the ability to bind to a site of tissue plasminogen activator (tPA) distal to its catalytic site and uncouple the beneficial clot-dissolving properties of tPA from its deleterious non-fibrinolytic effects.
T41029 Streptokinase

Streptokinase is a bacterial protein that acts as a plasminogen activator, commonly employed in the investigation of blood-clotting disorders. Its application extends to enhancing reperfusion blood flow after coronary artery occlusion.
T68682 Piriprost

Piriprost is a leukotriene inhibitor attenuates the smoke-induced increase in alveolar-capillary barrier permeability and decrease in plasminogen activator activity and causes a swelling of type I alveolar epithelium.
T72113 6-Aminocaproic acid hydrochloride

EACA hydrochloride,EACA hydrochloride ; Epsilon-Amino-n-caproic Acid hydrochloride ; 6-Aminohexanoic acid hydrochloride,6-Aminohexanoic acid hydrochloride,Epsilon-Amino-n-caproic Acid hydrochloride

6-Aminocaproic acid hydrochloride,一种单氨基羧酸,作为有效及口服活性的纤溶酶和纤溶酶原抑制剂,具备显著的抗纤溶能力。通过竞争性结合纤溶酶原上的赖氨酸残基,6-Aminocaproic acid hydrochloride 阻止血块溶解,抑制纤溶酶生成,减少纤维蛋白溶解,用于出血性疾病研究。
T35931 GGACK (hydrochloride)

GGACK is an inhibitor of urokinase-type plasminogen activator (uPA) and factor Xa (Kis = 1.8 and 8.7 μM, respectively).1,2 1.Kettner, C., and Shaw, E.The susceptibility of urokinase to affinity labeling by peptides of arginine chloromethyl ketoneBiochim. Biophys. Acta569(1)31-40(1979) 2.Kettner, C., and Shaw, E.The selective affinity labeling of factor Xa by peptides of arginine chloromethyl ketoneThromb. Res.22(5-6)645-652(1981)
T73701 Urokinase (peptidolytic)

Urokinase peptidolytic (Urokinase-type plasminogen activator) 是一种丝氨酸蛋白酶,是丝氨酸蛋白酶纤溶酶的一种非活性形式(酶原)。纤溶酶的激活可触发蛋白水解级联反应,进而参与血栓溶解或细胞外基质降解,涉及血管疾病和癌症相关研究。
TP2338 Cenupatide

UPARANT,Cenupatide trifluoroacetic acid salt,Ac-Arg-Aib-Arg-α(Me)Phe-NH2)

Cenupatide is a urokinase plasminogen activator receptor (uPAR) inhibitor. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of STZ-induced diabetes. Cenupatide reverted STZ-induced up-regula
T40614 LCKLSL

LCKLSL, an N-terminal hexapeptide, acts as a competitive inhibitor of annexin A2 (AnxA2), effectively preventing the binding of tissue plasminogen activator (tPA) to AnxA2 while also inhibiting the generation of plasmin. In addition, LCKLSL exhibits anti-angiogenic properties.
T11152 Edaravone-d5

MCI-186 D5

Others Others
Edaravone, a novel and potent free radical scavenger, effectively prevents MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator. Its deuterium-labeled variant, Edaravone D5, retains the original compound's attributes while offering isotopic labeling benefits.
T80859 Vitronectin

Vitronectin为一类多功能糖蛋白,广泛分布于血液及细胞外基质。该蛋白质与糖胺聚糖、胶原蛋白、纤溶酶原及尿激酶受体发生结合,并对纤溶酶原激活抑制剂1的抑制构象起稳定作用。Vitronectin常用于促进伤口愈合和肿瘤进展研究领域。
T80736 Z-Gly-Gly-Arg-AFC

Z-Gly-Gly-Arg-AFC为具有生物活性的肽类化合物,属于(纤溶酶原激活剂顶体碱底物,荧光Z-Gly-Gly-Arg-AFC)。
T68513 BSc2118

BSc2118 is a potent proteasome inhibitor. BSc2118 shows significant antimyeloma activity and may be considered as a promising agent in cancer drug development. BSc2118 is also a promising new candidate for stroke therapy, which may in addition alleviate recombinant tissue-plasminogen activator-induced brain toxicity.
TP2482 LCKLSL acetate

LCKLSL acetate(533902-29-3 free base)

Annexin A GPCR/G Protein
LCKLSL acetate 是一种竞争性膜联蛋白 A2 (AnxA2) 抑制剂。 LCKLSL acetate 有效抑制组织纤溶酶原激活剂 (tPA) 与 AnxA2 的结合和纤溶酶的产生。 LCKLSL acetate 具有抗血管生成作用。
T64287 Reteplase

Reteplase (BM 06.022) 是一种重组纤溶酶原 (plasminogen) 激活剂,由人组织型纤溶酶原激活剂的 kringle 2 和蛋白酶结构域构成。Reteplase 能够将纤溶酶原转化为纤溶酶,促使血栓溶解。Reteplase 通过 DNA 技术在大肠杆菌中产生的 t-PA 突变体,未糖基化。
T78015 LCKLSL hydrochloride

LCKLSL hydrochloride为N端六肽,作为膜联蛋白A2(AnxA2)的竞争性抑制剂,有效阻止组织纤溶酶原激活物(tPA)与AnxA2结合。此化合物还能够抑制纤溶酶生成,并表现出抗血管生成活性。

化合物

Plasminogen
Cat.No: T78018
Synonym:
Target:
ZK824190
Cat.No: T13408
Synonym:
Target: Others, Serine Protease
SK-216
Cat.No: T28788
Synonym: SK216.Plasminogen activator inhibitor-1 (PAI-1) inhibitor
Target:
TM5007
Cat.No: T8962
Synonym:
Target: PAI-1
TM5441
Cat.No: T4254
Synonym:
Target: PAI-1, Apoptosis
UK-371804
Cat.No: T3442
Synonym: UK371804
Target: PAI-1, Serine Protease
Upamostat
Cat.No: T13257
Synonym:
Target: PAI-1, Serine/threonin kinase, Serine Protease
TM5275 sodium
Cat.No: T4255
Synonym: TM5275 sodium salt
Target: PAI-1
Tiplaxtinin
Cat.No: T2030
Synonym: PAI-039,Tiplasinin
Target: PAI-1, Apoptosis
Aleplasinin
Cat.No: T29856
Synonym: PAZ 417,PAZ417,PAZ-417
Target: PAI-1
Benzamidine hydrochloride
Cat.No: T8362
Synonym: Benzamidine HCl,苄脒盐酸盐
Target: Serine/threonin kinase, Serine Protease
Cenupatide acetate
Cat.No: TP2338L
Synonym: Cenupatide acetate(1006388-38-0 Free base)
Target: Others
Aprotinin
Cat.No: T3359
Synonym: 抑酶肽,抑肽酶,Bovine Pancreatic Trypsin Inhibitor,Traskolan,Antilysin
Target: Others, Serine Protease, Influenza Virus, Proteasome
4-Aminobenzamidine dihydrochloride
Cat.No: T60248
Synonym: p-Aminobenzamidine dihydrochloride
Target: Serine Protease
5-trans-Prostaglandin E2
Cat.No: T71851
Synonym:
Target:
UKI-1
Cat.No: T13251
Synonym: UKI-1C
Target: Others
U46,195
Cat.No: T70734
Synonym:
Target:
XR 1853
Cat.No: T70417
Synonym:
Target:
UK-356202
Cat.No: T69751
Synonym:
Target:
IMD-1622
Cat.No: T68572
Synonym:
Target:
PS-519
Cat.No: T69890
Synonym:
Target:
Valyl-glycyl-arginine-4-nitroanilide
Cat.No: T68659
Synonym:
Target:
U 34599
Cat.No: T69319
Synonym:
Target:
Diaplasinin
Cat.No: T25915
Synonym: PAI-749,PAI749,PAI 749
Target:
ZK824859 hydrochloride (2271122-53-1 free base)
Cat.No: T13409L
Synonym: ZK824859 hydrochloride
Target: Others
UCD74A HCl
Cat.No: T70927
Synonym:
Target:
ZK824859
Cat.No: T13409
Synonym:
Target: Others
UK122
Cat.No: T41085
Synonym: UK122
Target:
THR-18
Cat.No: T70810
Synonym:
Target:
Streptokinase
Cat.No: T41029
Synonym:
Target:
Piriprost
Cat.No: T68682
Synonym:
Target:
6-Aminocaproic acid hydrochloride
Cat.No: T72113
Synonym: EACA hydrochloride,EACA hydrochloride ; Epsilon-Amino-n-caproic Acid hydrochloride ; 6-Aminohexanoic acid hydrochloride,6-Aminohexanoic acid hydrochloride,Epsilon-Amino-n-caproic Acid hydrochloride
Target:
GGACK (hydrochloride)
Cat.No: T35931
Synonym:
Target:
Urokinase (peptidolytic)
Cat.No: T73701
Synonym:
Target:
Cenupatide
Cat.No: TP2338
Synonym: UPARANT,Cenupatide trifluoroacetic acid salt,Ac-Arg-Aib-Arg-α(Me)Phe-NH2)
Target:
LCKLSL
Cat.No: T40614
Synonym:
Target:
Edaravone-d5
Cat.No: T11152
Synonym: MCI-186 D5
Target: Others
Vitronectin
Cat.No: T80859
Synonym:
Target:
Z-Gly-Gly-Arg-AFC
Cat.No: T80736
Synonym:
Target:
BSc2118
Cat.No: T68513
Synonym:
Target:
LCKLSL acetate
Cat.No: TP2482
Synonym: LCKLSL acetate(533902-29-3 free base)
Target: Annexin A
Reteplase
Cat.No: T64287
Synonym:
Target:
LCKLSL hydrochloride
Cat.No: T78015
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3876 Loureirin B

龙血素B,龙血素 B

PAI-1; ERK; Potassium Channel; JNK MAPK; Membrane transporter/Ion channel; Metabolism
Loureirin B 是从剑叶龙血树中分离到的一种黄酮,是 PAI-1抑制剂,IC50值为 26.10 μM。它抑制 KATP,以及 ERK 和 JNK 的磷酸化,具有抗糖尿病的功效。
T4S0592 Toddalolactone

(+)-Toddalolactone,飞龙掌血内酯,毛两面针素

PAI-1 Metabolism
Toddalolactone ((+)-Toddalolactone) 是一种Toddalia asiatica 的主要成分,能够抑制重组人纤溶酶原激活物抑制物-1(PAI-1)的活性, IC50=37.31 μM。
T0881 6-Aminocaproic acid

氨基己酸,EACA,6-氨基己酸,6-Aminohexanoic acid,Epsilon-Amino-n-caproic Acid,(6-)ε-​Aminocaproic acid

Others Others
6-Aminocaproic acid (EACA) 是一种单氨基羧酸,是一种有效的、具有口服活性的纤溶酶和纤溶酶原的抑制剂。它是一种有效的抗纤维蛋白溶解剂,能够竞争性结合纤溶酶原上的赖氨酸残基,防止血块溶解,并抑制纤溶酶的形成,减少纤维蛋白溶解。它可用于出血性疾病的研究。
T6S1699 Shogaol

[6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol

Lipoxygenase; Autophagy Autophagy; Metabolism
6-Shogaol (6-Shogaol) 是从生姜中分离的一种天然产物,具有抗癌、抗炎和抗氧化的多种生物活性。

天然产物

Loureirin B
Cat.No: T3876
Synonym: 龙血素B,龙血素 B
Target: PAI-1, ERK, Potassium Channel, JNK
Toddalolactone
Cat.No: T4S0592
Synonym: (+)-Toddalolactone,飞龙掌血内酯,毛两面针素
Target: PAI-1
6-Aminocaproic acid
Cat.No: T0881
Synonym: 氨基己酸,EACA,6-氨基己酸,6-Aminohexanoic acid,Epsilon-Amino-n-caproic Acid,(6-)ε-​Aminocaproic acid
Target: Others
Shogaol
Cat.No: T6S1699
Synonym: [6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol
Target: Lipoxygenase, Autophagy
TargetMol Loading
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