Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7137 |
I-191
|
Protease-activated Receptor | GPCR/G Protein |
I-191 是选择性有效的蛋白酶激活受体 2 拮抗剂。 | |||
T7625 |
TRAP-6
PAR-1 agonist peptide,Thrombin Receptor Activator Peptide 6,TRAP-6(2TFA) |
Protease-activated Receptor | GPCR/G Protein |
TRAP-6 (Thrombin Receptor Activator Peptide 6) 是一种多肽片段,是选择性的蛋白酶激活受体 1 (PAR1) 激动剂,通过凝血酶受体激活人血小板。 | |||
TQ0012 |
AZ3451
|
Protease-activated Receptor | GPCR/G Protein |
AZ3451 是蛋白酶激活受体 2 的变构拮抗剂,IC50值为 23 nM。 | |||
T1986 |
Atopaxar
E5555,ER-172594-00 |
Protease-activated Receptor | GPCR/G Protein |
Atopaxar (E5555) 是一种高效、可口服的,选择性的,可逆的凝血酶受体蛋白酶激活受体-1 (PAR-1) 拮抗剂。它是一种抗血小板剂,能干扰血小板信号,可用于动脉粥样硬化血栓性疾病的研究。 | |||
T12870 |
SCH79797 dihydrochloride
|
Apoptosis; Others; Protease-activated Receptor | Apoptosis; GPCR/G Protein; Others |
SCH79797 dihydrochloride 是一种有效的特异性蛋白酶激活受体 1 (PAR1) 拮抗剂,IC50 为 70 nM,Ki 为 35 nM。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用。 | |||
TP1046 |
SLIGRL-NH2
Protease-Activated Receptor-2 Activating Peptide |
Protease-activated Receptor | GPCR/G Protein |
SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) 为一种蛋白酶激活受体-2 (PAR-2) 激动剂,具有诱导非组胺能性瘙痒的功能。 | |||
T2370 |
AC-55541
AOB2796 |
Proteasome; Protease-activated Receptor | GPCR/G Protein; Proteases/Proteasome; Ubiquitination |
AC-55541 (AOB2796) 是高选择性的蛋白酶激活受体 2(PAR2)激动剂,pEC50为6.7。它在 PI 水解测定和 Ca2+动态测定中的pEC50值为 5.9 和 6.6,在体内表现出伤害感受器活性。 | |||
T7013 |
Vorapaxar
SCH 530348,MK-5348,沃拉帕沙 |
Protease-activated Receptor | GPCR/G Protein |
Vorapaxar (MK-5348) 是抗血小板药物,是一种选择性、口服活性和竞争性的凝血酶受体蛋白酶激活受体(PAR-1)拮抗剂,Ki 值为 8.1 nM。它靠剂量依赖性抑制凝血酶受体激活肽 (TRAP) 诱导的血小板聚集。 | |||
T1893 |
Parmodulin 2
ML 161 |
Protease-activated Receptor | GPCR/G Protein |
Parmodulin 2 (ML 161) 是一种蛋白酶激活受体 1(PAR1) 变构抑制剂,IC50为 0.26 μM。它是蛋白酶激活受体 1 (PAR1) 介导的血小板活化的抑制剂,可以抑制体外血小板聚集和体内血小板血栓形成。 | |||
T8917 |
PAR-2-IN-1
IUN76750,8-(叔丁基)-6-氯咪唑并[1,2-B]吡啶-2-羧酸甲酯 |
Protease-activated Receptor | GPCR/G Protein |
PAR-2-IN-1 (IUN76750) 是一种 PAR-2 信号通路抑制剂,具有抗炎和抗癌作用。 | |||
T3098 |
Vorapaxar sulfate
SCH 530348 sulfate,Zontivity,vorapaxar monosulfate,沃拉帕沙 |
Protease-activated Receptor | GPCR/G Protein |
Vorapaxar sulfate (Zontivity) 是一种选择性、口服活性和竞争性的凝血酶受体蛋白酶激活受体(PAR-1)拮抗剂,Ki 值为 8.1 nM。它剂量依赖性抑制凝血酶受体激活肽 (TRAP) 诱导的血小板聚集,是抗血小板药物。 | |||
T7496 |
Thrombin Receptor Activator for Peptide 5 (TRAP-5)
Thrombin Receptor Activator for Peptide |
Protease-activated Receptor | GPCR/G Protein |
Thrombin Receptor Activator for Peptide 5 (TRAP-5) 也称为凝血因子 II 受体 (1-5) 或蛋白酶激活受体 1 (1-5),用于研究冠心病 (CHD)。 | |||
T7513 |
Protease-Activated Receptor-2, amide
蛋白酶活化的受体-2,酰胺,SLIGKV-NH2,H-丝氨酰亮氨酰异亮氨酰甘氨酰赖氨酰缬氨酰NH2 |
Protease-activated Receptor | GPCR/G Protein |
Protease-Activated Receptor-2, amide (SLIGKV-NH2) 是 PAR2 的激动剂,IC50为 10.4 M。 | |||
TP1065 |
PAR-4 Agonist Peptide, amide TFA
PAR-4-AP (TFA),AY-NH2 (TFA) |
Protease-activated Receptor | GPCR/G Protein |
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP (TFA)) 是一种蛋白酶激活受体 4 (PAR-4) 激动剂,对 PAR-1 或 PAR-2 均无影响,其作用可被 PAR-4 拮抗剂阻断。 | |||
T1986L |
Atopaxar Hydrobromide
|
Protease-activated Receptor | GPCR/G Protein |
Atopaxar hydrobromide 是可口服的,高效选择性的可逆凝血酶受体蛋白酶激活受体-1 拮抗剂。它是一种抗血小板剂,能干扰血小板信号,用于动脉粥样硬化血栓性疾病的研究。 | |||
T4186 |
AC-264613
AC264613 |
Protease-activated Receptor | GPCR/G Protein |
AC-264613 是一种选择性蛋白酶激活受体 (PAR-2) 激动剂,pEC50为 7.5。 | |||
T7573 |
TFLLR-NH2
TFLLR-NH2(2TFA) |
Protease-activated Receptor | GPCR/G Protein |
TFLLR-NH2 是选择性的一种PAR1激动剂,EC50值为1.9 μM。 | |||
T7380 |
Protease-Activated Receptor-4
蛋白酶活化的受体-4 |
Protease-activated Receptor | GPCR/G Protein |
Protease-Activated Receptor-4 是蛋白酶激活受体 4 激动剂,具有抗血小板治疗。 | |||
T7623 |
PAR-4 Agonist Peptide, amide
AY-NH2,PAR-4 Agonist Peptide, amide(2TFA),PAR-4-AP |
Protease-activated Receptor | GPCR/G Protein |
PAR-4 Agonist Peptide, amide (AY-NH2) 是蛋白酶激活受体 4 (PAR-4) 的激动剂,对 PAR-1 或 PAR-2 均无影响,其作用可被 PAR-4 拮抗剂阻断。 | |||
T80240 |
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
|
||
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2是一类具有生物活性的肽,作为蛋白酶激活受体1 (PAR-1) 的选择性激动剂,其特异性优于PAR-2。该肽通过HEK293细胞进行的基于细胞的钙信号传导测定确认了其对PAR-1的高特异性,并可用于研究PAR-1在体内的激活。PAR-1除了介导凝血酶的多种细胞作用外,还与PAR-4协作,参与调控凝血酶诱导的被分类为“凝血型”的肝细胞癌。 | |||
T36717 |
RWJ-56110 dihydrochloride
|
||
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap... | |||
T36101 |
Psychotridine
|
||
Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg/kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Pol... |