43
3
15
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T72025 |
PCSK9-IN-10
|
Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism |
PCSK9-IN-10 是一种有效的,具有口服活性的PCSK9抑制剂,IC50值为 6.4 µM。PCSK9-IN-10 增加LDLR 蛋白的表达并降低 PCSK9 的表达。PCSK9-IN-10 可减缓动脉粥样硬化进展。PCSK9-IN-10 具有研究高脂血症的潜力。 | |||
T67776 |
PCSK9-IN-11
|
Others | Others |
PCSK9-IN-11 (compound 5r) 是口服有效的 PCSK9 抑制剂。 PCSK9-IN-11 在 HepG2 细胞中抑制 PCSK9 转录活性 (IC50= 5.7 μM)。 PCSK9-IN-11 可以增加 LDL 受体 (LDLR) 蛋白水平,可用于动脉粥样硬化研究。 | |||
T64362 |
AZD0780
PCSK9-IN-12,EX-A6975 |
Others | Others |
AZD0780 (EX-A6975)表现出对PCSK9的结合亲和力(Kd<200nM)。AZD0780在胆固醇代谢方面具有研究价值。 | |||
T39528 |
PCSK9-IN-2
PCSK9-IN-2 |
||
PCSK9-IN-2 is a newly developed small molecule that effectively inhibits the protein-protein interaction (PPI) between PCSK9 and LDLR. It has been found to have a potent inhibitory activity with an IC50 value of 7.57 μM. | |||
T39685 |
PCSK9 degrader 1
|
||
PCSK9 degrader 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) degrader. PCSK9 degrader 1 does not affect PCSK9 function. | |||
T13813 |
PCSK9 ligand 1
|
Others | Others |
PCSK9 ligand 1 is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9(Ki of 107 nM). | |||
T60541 |
PCSK9 modulator-2
|
||
PCSK9 modulator-2 (Compound 1) 是一种有效的PCSK9调节剂(EC50 = 202 nM), 具有用于高脂血症的研究潜力。PCSK9 是降低低密度脂蛋白胆固醇 (LDL-C) 的靶点。 | |||
T60764 |
PCSK9 modulator-4
|
||
PCSK9 modulator-4 (Compound 21) 是可以用于高血脂研究的,PCSK9的有效调节剂 (EC 50 = 0.15 nM)。PCSK9 是得到验证的一种降低低密度脂蛋白胆固醇 (LDL-C) 的靶标。 | |||
T79030 |
PCSK9-IN-14
|
||
PCSK9-IN-14 (compound Ia-8)为高效的PCSK9抑制剂。 | |||
T60646 | PCSK9 modulator-3 | ||
PCSK9 modulator-3 (Compound 13) 是PCSK9的有效调节剂,EC50值为 2.46 nM,在高脂血症研究中具有潜力。PCSK9 是已证实的降低低密度脂蛋白胆固醇 (LDL-C) 的靶点。 | |||
T79052 | PCSK9-IN-16 | ||
PCSK9-IN-16,有效的PCSK9抑制剂,用于治疗高胆固醇血症及其他心血管疾病。 | |||
T74167 | PCSK9-IN-3 | ||
PCSK9-IN-3为新一代口服高效三环肽类PCSK9抑制剂,特征为新型化合物。 | |||
T79239 |
PCSK9-IN-19
|
||
PCSK9-IN-19 (Compound 1)作为一种PCSK9抑制剂,用于研究高LDL胆固醇水平及预防冠状动脉疾病。 | |||
T9920 |
Evolocumab
|
Others | Others |
Evolocumab 是人源化单克隆抗体PCSK9的抑制剂。它与循环的 PCSK9 蛋白结合,使得PCSK9与 LDLR 结合受到抑制。它可用研究于高胆固醇血症以及动脉粥样硬化性心血管疾病的研究。 | |||
T79053 | PCSK9-IN-17 | ||
PCSK9-IN-17作为PCSK9抑制剂,主要应用于胆固醇代谢研究。 | |||
T75147 | PCSK9-IN-18 | ||
PCSK9-IN-18 (compound 188)是一种有效的 PCSK9抑制剂,KD 值为 <200 nM[1]。 | |||
T79051 |
PCSK9-IN-15
|
||
PCSK9-IN-15(化合物5)是一种高效PCSK9抑制剂,亲和力强(KD<200 nM)。该化合物与胆固醇代谢相关,可调控低密度脂蛋白胆固醇(LDL-C)水平,适用于研究降低胆固醇及血脂异常。 | |||
T81535 |
PCSK9-IN-20
|
||
PCSK9-IN-20(Compound 3i)作为一种PCSK9抑制剂,具有IC50为 3.96 µM,能有效降低体外PCSK9水平并提升LDLR蛋白表达。 | |||
T73008 | PCSK9-IN-13 | ||
PCSK9-IN-13 是一种有效的PCSK9抑制剂, 可通过与 PCSK9 结合作用来拮抗低密度脂蛋白(LDL) 受体结合,其IC50值为 537 nM。 | |||
T70068 |
AT-1015 hydrochloride monohydrate
|
||
AT-1015 hydrochloride monohydrate is a serotonin (5-HT)2 receptor antagonist that blocks vascular and platelet 5-HT2A receptors. | |||
T4058 |
R-IMPP
|
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
R-IMPP 是抗 PCSK9分泌的药物 (IC50=4.8 μM),靶向作用于 80S 核糖体,抑制 PCSK9 蛋白的翻译。 | |||
TP1881L1 |
Pep 2-8 ammonium salt(1541011-97-5 free base)
|
Others | Others |
Pep 2-8 ammonium salt(1541011-97-5 free base) 是 Proprotein 转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 抑制剂。 PCSK9 与 LDL 受体结合的强效抑制剂 (IC50 = 0.8 μM)。恢复用 PCSK9 处理的 HepG2 细胞中的 LDL 摄取。 | |||
T9276 |
SBC-115337
|
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
SBC-115337 是苯并呋喃化合物,也是 PCSK9抑制剂 (IC50:0.5 μM) 。 | |||
T8645 |
PF-06446846
|
Others | Others |
PF-06446846 是口服有活性的 PCSK9抑制剂。它能够在密码子区域附近阻断 80S ribosome,选择性地直接抑制 PCSK9 的翻译。 | |||
T16491 |
PF-06446846 hydrochloride
|
Others | Others |
PF-06446846 hydrochloride 是一种口服活性高、高选择性PCSK9(前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型)翻译抑制剂。它通过在密码子34附近诱导核糖体暂停来抑制PCSK9。 | |||
T4524 |
SBC-110736
SBC110736 |
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
SBC-110736 是一种蛋白转化酶枯草杆菌蛋白酶 9 型 (PCSK9) 抑制剂。 | |||
T2626 |
SBC-115076
SBC115076 |
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
SBC-115076 是前蛋白转化酶枯草杆菌蛋白酶/ kexin 9型(PCSK9)抑制剂。其中PCSK9 是一种前蛋白转化酶,在 LDL 受体代谢中的重要物质。 | |||
T76739 |
Bococizumab
RN316,PF-04950615 |
Others | Others |
Bococizumab(PF-04950615) 是一种针对PCSK9的人源化mAb,也是一种在肝脏中合成PCSK9的抑制剂,可降低低密度脂蛋白胆固醇 (LDL-C) 在血液中的含量。Bococizumab 可用于治疗高胆固醇血症。 | |||
T9916 |
Alirocumab
|
Others | Others |
Alirocumab 是 PCSK9的人单克隆抗体。它能够特异性结合肝脏低密度脂蛋白 (LDL) 受体的下调剂 PCSK9,增强肝脏结合 LDL-胆固醇 (LDL-C) 的能力,降低血液中的 LDL-C 水平。它可用于研究高胆固醇血症。 | |||
TP1881 |
Pep2-8
Pep 2-8 |
||
Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9. | |||
T78718 | Dim16 | ||
Dim16是一种同时抑制PCSK9和HMG-CoAR的化合物,其对PCSK9的IC50为19 nM,并且能够阻断PCSK9与LDLR的结合,此作用的IC50为0.8 nM。Dim16还能提升HepG2细胞对LDL的吸收。 | |||
T74573 |
Bezeparsen
|
||
Bezeparsen 是一种 PCSK9 合成抑制剂。 | |||
T74730 | SPC4061 | ||
SPC4061 是一种反义核苷酸,是有效的 PCSK9抑制剂。SPC4061 靶向 PCSK9 的锁定核酸 (LNA),可用于高胆固醇血症和相关疾病的研究。 | |||
T70069 |
MDK6465
|
||
MDK6465, also known as PCSK9-IN-8b, is a novel liver-targeted inhibitor of ribosomal synthesis of proprotein convertase subtilisin/kexin type 9 (PCSK9). MDK6465 has CAS#1900686-46-5. the last 4 digits are used in its name. | |||
T78013 |
Pep2-8 TFA
|
||
Pep2-8是增强PCSK9拮抗活性的肽,作用于前蛋白转化酶枯草杆菌蛋白酶/可辛9型(PCSK9)。 | |||
T77014 | Frovocimab | ||
Frovocimab (LY 3015014)为一种人源化IgG4单克隆抗体(mAb),其功能为中和PCSK9,通过抑制PCSK9与LDL受体(LDLR)的结合,促使已结合的PCSK9正常进行蛋白水解切割。 | |||
T77140 | Ralpancizumab | ||
Ralpancizumab 是一种 PCSK9选择性抑制剂,在出血性中风中有潜在应用。 | |||
T72221 |
PF-06815345 hydrochloride
|
||
PF-06815345 hydrochloride 是一款口服有效的PCSK9抑制剂,其IC50值为13.4 μM。在小鼠体内,能显著降低PCSK9水平。 | |||
T80608 |
Ebronucimab
AK102 |
||
Ebronucimab (AK102)为一种针对PCSK9的IgG1-λ2单克隆抗体,其主要源自经过工程化改造的CHO DG44细胞系。 | |||
T77144 | Recaticimab | ||
Recaticimab (SHR-1209) 是一种针对 PCSK9 的人源化单克隆抗体。该药物通过结合 PCSK9 并促进其降解,增加肝细胞表面的低密度脂蛋白 (LDL) 受体数量,从而有效降低血浆 LDL 水平,实现降低血脂的效果。Recaticimab 对于治疗高胆固醇血症显示出潜在价值。 | |||
T77113 | Ongericimab | ||
Ongericimab (JS002),一种人源化抗PCSK9单克隆抗体,可用于高胆固醇血症和高脂血症的研究,具有降脂功效。 | |||
T16322 |
Nicodicosapent
|
Others | Others |
Nicodicosapent is a fatty acid niacin conjugate. It is also an inhibitor of the sterol regulatory element-binding protein (SREBP). The sterol regulatory element-binding protein (SREBP) is a key regulator of cholesterol metabolism proteins such as PCSK9, H | |||
T77058 | Lerodalcibep | ||
Lerodalcibep (LIB003) 是一种重组融合蛋白,由PCSK9结合域 (adnectin) 与人血清白蛋白组成。作为降脂剂,Lerodalcibep 适用于高胆固醇血症和心血管疾病的研究。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T75545 | PCSK9-IN-9 | ||
PCSK9-IN-9 是一种天然来源的异香豆素。PCSK9-IN-9 可抑制原蛋白转化酶枯草菌素 kexin 型 9 (PCSK9)、IDOL 和 SREBP2的 mRNA 表达水平。PCSK9-IN-9 抑制 PCSK9的 IC50为 11.9 μM。 | |||
TN2082 |
Pinostrobin
|
Beta Amyloid; IL Receptor; Serine/threonin kinase; TNF | Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; Metabolism; Neuroscience |
Pinostrobin 是一种 PCSK9抑制剂,可抑制 PCSK9 的催化活性。它是能够在多种植物中发现的黄酮类化合物,并具有抗氧化,抗炎,抗癌和神经保护作用。它是有前景的胆固醇调节和脂质管理剂。 | |||
T77289 | 5-O-Methylembelin | ||
5-O-Methylembelin 是一种天然异香豆素,可抑制PCSK9、低密度脂蛋白受体 (IDOL) 和甾醇调节元件结合蛋白 2 (SREBP2) mRNA 的表达。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPK-00483 |
PCSK9 Protein, Cynomolgus, Recombinant (His)
PCSK9 |
Cynomolgus | HEK293 Cells |
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene in humans on chromosome 1.The first two PCSK9 inhibitors, alirocumab and evolocumab, were approved as once every two week injections, by the U.S. Food and Drug Administration in 2015 for lowering LDL-particle concentrations when statins and other drugs were not sufficiently effective or poorly tolerated. | |||
TMPJ-00443 |
PCSK9 Protein, Macaca nemestrina, Recombinant (His)
Proprotein Convertase Subtilisin/Kexin Type 9,P... |
Macaca nemestrina | HEK293 Cells |
Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) is a secretory subtilase belonging to the proteinase K subfamily. PCSK9 is synthesized as a soluble zymogen that undergoes autocatalytic intramolecular processing in the ER , the pro domain and mature chain secrete together through noncovalent interactions. PCSK9 binds with low-density lipoprotein receptor (LDLR) and plays a major regulatory role in cholesterol homeostasis. PCSK9 also plays a role in the neural development. | |||
TMPY-04966 |
PCSK9 Protein, Human, Recombinant (D374Y, His)
LDLCQ1,NARC-1,PC9,NARC1,HCHOLA3,proprotein converta... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (D374Y, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 72.5 kDa and the accession number is Q8NBP7-1. | |||
TMPJ-00368 |
PCSK9 Protein, Human, Recombinant (Avi), Biotinylated
Subtilisin/Kexin-Like Protease PC9,PC9,NAR... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (Avi), Biotinylated is expressed in HEK293 mammalian cells with C-Avi tag. The predicted molecular weight is 19&65 KDa and the accession number is Q8NBP7. | |||
TMPY-05131 |
PCSK9 Protein, Human, Recombinant (His & Avi), Biotinylated
NARC-1,PC9,LDLCQ1,NARC1,FH3,proprotein convertase s... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with His and Avi tag. The predicted molecular weight is 74.3 kDa and the accession number is Q8NBP7-1. | |||
TMPJ-00369 |
PCSK9 Protein, Human, Recombinant (His & HA & Avi), Biotinylated
Subtilisin/Kexin-Like Protease PC9,PCSK |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (His & HA & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-8xHis-HA-Avi tag. The predicted molecular weight is 18 and 58-70 and 90-150 KDa and the accession number is Q8NBP7. | |||
TMPY-00408 |
PCSK9 Protein, Human, Recombinant (D374Y & V474I & G670E, His)
FH3,proprotein convertase subtilisin/kexin type 9,L... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (D374Y & V474I & G670E, His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 72.6 kDa and the accession number is AAV67948.1. | |||
TMPY-05218 |
PCSK9 Protein, Human, Recombinant (mFc)
HCHOLA3,PC9,proprotein convertase subtilisin/kexin ... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (mFc) is expressed in HEK293 mammalian cells with mFc tag. The predicted molecular weight is 97.4 kDa and the accession number is Q8NBP7-1. | |||
TMPY-00995 |
PCSK9 Protein, Rhesus, Recombinant (His)
proprotein convertase subtilisin/kexin type 9 |
Rhesus | HEK293 Cells |
PCSK9 Protein, Rhesus, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 72.7 kDa and the accession number is A8T666. | |||
TMPY-05217 |
PCSK9 Protein, Mouse, Recombinant (mFc)
HCHOLA3,Narc1,AI415265,AI747682,FH3,proprotein convertase su... |
Mouse | HEK293 Cells |
PCSK9 Protein, Mouse, Recombinant (mFc) is expressed in HEK293 mammalian cells with mFc tag. The predicted molecular weight is 97.6 kDa and the accession number is Q80W65. | |||
TMPY-01565 |
PCSK9 Protein, Rat, Recombinant (His)
proprotein convertase subtilisin/kexin type 9 |
Rat | HEK293 Cells |
PCSK9 Protein, Rat, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 72.8 kDa and the accession number is A6JYM6. | |||
TMPY-01245 |
PCSK9 Protein, Mouse, Recombinant (His)
proprotein convertase subtilisin/kexin type 9,AI747... |
Mouse | HEK293 Cells |
PCSK9 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 72.6 kDa and the accession number is Q80W65. | |||
TMPY-05270 |
PCSK9 Protein, Human, Recombinant (D374Y, mFc), Biotinylated
FH3,NARC-1,PC9,LDLCQ1,proprotein convertase subtili... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (D374Y, mFc), Biotinylated is expressed in HEK293 mammalian cells with mFc tag. The predicted molecular weight is 97.5 kDa and the accession number is Q8NBP7-1. | |||
TMPY-05199 |
PCSK9 Protein, Human, Recombinant (D374Y, mFc)
PC9,proprotein convertase subtilisin/kexin type |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (D374Y, mFc) is expressed in HEK293 mammalian cells with mFc tag. The predicted molecular weight is 97.5 kDa and the accession number is Q8NBP7-1. | |||
TMPY-05114 |
PCSK9 Protein, Human, Recombinant (D374Y & V474I & G670E, His), Biotinylated
LDLCQ1,NARC-1,PC9,FH3,NARC1,HCHOLA3,proprotein conv... |
Human | HEK293 Cells |
PCSK9 Protein, Human, Recombinant (D374Y & V474I & G670E, His), Biotinylated is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 72.6 kDa and the accession number is Q8NBP7-1. |