目录号 | 产品详情 | 靶点 | |
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T9189 | Complement System | ||
Iptacopan hydrochloride (LNP023 hydrochloride) 是一种可口服、高效和高选择性的因子 B 抑制剂,IC50 为 10 nM。 LNP023 显示与人因子 B 的直接、可逆和高亲和力结合,KD 为 7.9 nM。 | |||
T76867 | Complement System | ||
Ravulizumab (ALXN1210) 是一种靶向补体因子 5 的人源化单克隆抗体,它以高亲和力特异性结合人补体蛋白 C5,可阻断补体激活。Ravulizumab 可用于预防和治疗阵发性睡眠性血红蛋白尿症、非典型溶血性尿毒症综合征和重症肌无力。 | |||
T15257 | Calcium Channel | ||
Etripamil (MSP-2017) 是一种短效L 型钙通道拮抗剂,可用于治疗阵发性室上性心动过速的研究。它通过抑制房室结细胞中钙慢通道的钙离子流入,显示房室结传导并延长房室结不应期 | |||
T8509 | Complement System | ||
Danicopan (ACH-4471) 是一种可口服的小分子 D 因子选择性抑制剂,对人 D 因子具有高结合亲和力,Kd 值为 0.54 nM。 它可抑制补体替代途径 (APC) 的活性,具有阻断阵发性夜间血红蛋白尿 (PNH) 和非典型溶血性尿毒症综合征 (aHUS) 的补体替代途径的潜力。 | |||
T21391 | |||
Flecainide acetate is a class Ic antiarrhythmic agent, it is used to treat a variety of cardiac arrhythmias including paroxysmal atrial fibrillation, paroxysmal supraventricular tachycardia, and ventricular tachycardia. It works by regulating the flow of | |||
T77190 | |||
Crovalimab (SKY59; RO7112689)是一种人源化抗C5抗体,其通过pH依赖性机制发挥作用,其KD值在pH 7.4时为15.2nM,在pH 5.8时为16.8μM。该化合物还以高亲和力结合于人FcRn(KD: 17μM; pH 6.0)。通过阻断C5转化酶对C5的切割及抑制C5变体(p.Arg885His)的活性,Crovalimab能够显著抑制补体系统中经典途径(CP)、凝集素途径(LP)以及旁路途径(AP)中C5b-9的形成。因此,Crovalimab展现出作为研究阵发性睡眠性血红蛋白尿(PNH)及其他补体介导疾病的潜力。 | |||
T64692 | |||
Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute to the development of alcohol-induced fatty liver and its consequences[4].AMY-101 TFA (Cp40 TFA) is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). It shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[5].a daily subcutaneous dose of AMY-101 (4 mg/kg bodyweight) was protective against NHP periodontitis, suggesting that patients treated for systemic disorders (e.g., paroxysmal nocturnal hemoglobinuria) can additionally benefit in terms of improved periodontal condition[6].Plasma concentrations of both C3 and Cp40 were measured periodically and complete saturation of plasma C3 was confirmed. No differences in hematological, biochemical, or immunological parameters were identified in the blood or tissues of animals treated with Cp40 when compared to those injected with vehicle alone. Further, skin wounds showed no signs of infection in those treated with Cp40.Cp40 treatment was associated with a trend toward accelerated wound healing when compared with the control group. In addition, a biodistribution study in a rhesus monkey indicated that the distribution of Cp40 in the body is associated with the presence of C3, concentrating in organs that accumulate blood and produce C3[7]. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-02266 | CD59a Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
Protectin, a complement regulatory protein, also known as CD59, or MIRL (membrane inhibitor of reactive lysis) is a small protein that inhibits the complement membrane attack complex by binding C5b678 and preventing C9 from binding and polymerizing. The amino-terminal 25 amino acids represented a typical signal peptide sequence and the carboxy-terminal hydrophobic amino acids were characteristic for phosphatidylinositol-anchored proteins. It was found that the CD59/Protectin antigen is a small protein sometimes associated with larger components (45 and 80 kD) in urine. CD59/Protectin antigen was released from the surface of transfected COS cells by phosphatidylinositol-specific phospholipase C, demonstrating that it is attached to the cell membrane by means of a glycolipid anchor; it is therefore likely to be absent from the surface of affected erythrocytes in the disease paroxysmal nocturnal hemoglobinuria.
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TMPY-01854 | DPP10 Protein, Human, Recombinant (His) | Human | HEK293 | ||
Inactive dipeptidyl peptidase 1, also known as Dipeptidyl peptidase IV-related protein 3, Dipeptidyl peptidase X, Dipeptidyl peptidase-like protein 2, DPRP-3, DPL2 and DPP1, is a single-pass type II membrane protein which belongs to thepeptidase S9B family.DPPIV subfamily. It may modulate cell surface expression and activity of the potassium channels KCND1 and KCND2. DPP1 / DPRP3 has no detectable protease activity, most likely due to the absence of the conserved serine residue normally present in the catalytic domain of serine proteases. However, it does bind specific voltage-gated potassium channels and alters their expression and biophysical properties. Genetic variations in DPP1 are associated with susceptibility to asthma (ASTHMA). The most common chronic disease affecting children and young adults. It is a complex genetic disorder with a heterogeneous phenotype, largely attributed to the interactions among many genes and between these genes and the environment. It is characterized by recurrent attacks of paroxysmal dyspnea, with weezing due to spasmodic contraction of the bronchi.
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TMPY-02503 | CD59a Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 | ||
Protectin, a complement regulatory protein, also known as CD59, or MIRL (membrane inhibitor of reactive lysis) is a small protein that inhibits the complement membrane attack complex by binding C5b678 and preventing C9 from binding and polymerizing. The amino-terminal 25 amino acids represented a typical signal peptide sequence and the carboxy-terminal hydrophobic amino acids were characteristic for phosphatidylinositol-anchored proteins. It was found that the CD59/Protectin antigen is a small protein sometimes associated with larger components (45 and 80 kD) in urine. CD59/Protectin antigen was released from the surface of transfected COS cells by phosphatidylinositol-specific phospholipase C, demonstrating that it is attached to the cell membrane by means of a glycolipid anchor; it is therefore likely to be absent from the surface of affected erythrocytes in the disease paroxysmal nocturnal hemoglobinuria.
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