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21

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T38332 Complement factor D-IN-2

Complement System Immunology/Inflammation
Complement factor D-IN-2 是 omplement factor D 的有效抑制剂,在替代补体途径的早期和关键时刻靶向 factor D 并抑制补体级联反应。Complement factor D-IN-2在自身免疫疾病的方面有研究的价值。
TP1304 Compstatin

坎普他汀

Complement System Immunology/Inflammation
Compstatin 是一种环状十三肽,是补体系统 C3的特异性抑制剂。它只抑制灵长类补体系统的激活,可结合到狒狒的 C3,并对狒狒血液中的蛋白水解裂解具有抗性。它对补体经典途径和旁路途径的 IC50值分别为 63 和 12 μM。
T9915 Eculizumab

Complement System Immunology/Inflammation
Eculizumab 是针对补体 C5 的长效人源化单克隆抗体。它对 C5 裂解为 C5a 和 C5b 具有抑制作用,并抑制了末端补体系统的部署,其中包括膜攻击复合物的形成。它可用于溶血的研究。
T8509 Danicopan

ACH-4471

Complement System Immunology/Inflammation
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。
T9189 Iptacopan hydrochloride

Iptacopan HCl,LNP023 hydrochloride

Complement System Immunology/Inflammation
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。
T9316 JR14a

5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-l-arginine hydrochloride

Complement System Immunology/Inflammation
JR14a (5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-l-arginine hydrochloride) 是补体C3a 受体噻吩拮抗剂,可抑制 C3aR 介导的炎症,对人 C3a 受体的选择性高于 C5a 受体。
T12851 SB290157 trifluoroacetate

Complement System Immunology/Inflammation
SB290157 trifluoroacetate 是一种选择性 C3a 受体拮抗剂,IC50值为200 nM。
T3638 Leukadherin-1

Integrin; Complement System Cytoskeletal Signaling; Immunology/Inflammation
Leukadherin-1 是 CD11b/CD18 的变构激活剂,可增加 CD11b/CD18 依赖性细胞对纤维蛋白原的粘附,减少白细胞运动和跨内皮迁移,具有抗炎作用。
T17250 W-54011

ROS; Complement System Immunology/Inflammation
W-54011 是口服有效的非肽 C5a 受体拮抗剂,抑制125I 标记的 C5a 与人嗜中性白细胞的结合,Ki 为 2.2 nM。它还抑制C5a 诱导的人嗜中性粒细胞的细胞内 Ca2+动员,趋化性和ROS 的生成,IC50分别为 3.1 nM、2.7 nM 和1.6 nM。
T7776 ADH-503

GB1275

Complement System Immunology/Inflammation
ADH-503 (GB1275) 是一种可口服的变构CD11b 激动剂,可以导致与肿瘤相关的巨噬细胞重新极化,可减轻骨髓细胞的免疫抑制,并增强树突状细胞的反应。
T1076 Dexamethasone

MK 125,Prednisolone F,NSC 34521,Hexadecadrol,地塞米松

Glucocorticoid Receptor; Mitophagy; IL Receptor; SARS-CoV; Antibacterial; Antibiotic; Autophagy; Complement System Autophagy; Endocrinology/Hormones; Immunology/Inflammation; Microbiology/Virology
Dexamethasone (Hexadecadrol) 是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。Dexamethasone 具有抗炎和免疫抑制活性,可诱导自噬。Dexamethasone 抑制 LPS 诱导的巨噬细胞炎症反应。
T7497 C3a (70-77)

Complement 3a (70-77),C3a 70-77

Complement System Immunology/Inflammation
C3a (70-77) 是对应于 C3a 的 COOH 末端的八肽。
T13379 (Z)-Leukadherin-1

ADH-503 free base

Complement System Immunology/Inflammation
(Z)-Leukadherin-1 (ADH-503 free base) 是 CD11b 的变构激动剂。
T38287 C3a Receptor Agonist

C3a receptor agonist 1,C3a受体激动剂,Complement 3a Receptor Agonist

Complement System Immunology/Inflammation
C3a Receptor Agonist (C3a receptor agonist 1) 结合免疫系统补体途径中的G 蛋白偶联C3a 受体(C3aRs)。在肠缺血再灌注损伤模型中,C3aR 的激活可防止中性粒细胞动员。C3aRs 在成年小鼠的神经祖细胞和未成熟神经元上表达。C3a 在体外刺激神经祖细胞的分化。
T38951 Isatuximab

SAR-650984,hu38SB19,Isatuximab-irfc

Apoptosis; CD38 Apoptosis; Immunology/Inflammation
Isatuximab 是一种在血液系统恶性细胞中靶向跨膜受体和胞外酶 CD38 的单克隆抗体,是在多发性骨髓瘤中高度表达的蛋白。Isatuximab 具有抗肿瘤活性、抗体依赖性细胞介导的细胞毒性、补体依赖性细胞毒性、抗体依赖性细胞吞噬作用,可在无交联情况下直接诱导细胞凋亡 (apoptosis)。Isatuximab 对 CD38 胞外酶活性有抑制作用,这与许多细胞功能有关。
T11269 FD-IN-1

Others Others
FD-IN-1 is a factor D (FD) inhibitor with an IC50 of 12 nM.FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5μM, respectively. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system.
TP1866 β-Amyloid (1-11)

β-amyloid 1-11

Anionic interaction of Beta-amyloid (1-11) with Factor XII is suspected to cause massive activation of the C4 (complement 4) system in the cerebrospinal fluid of Alzheimer’s disease patients.
T75775 Compstatin TFA

Compstatin TFA是一种含有13个残基的环肽,作为补体系统C3的高效抑制剂,显示出物种特异性。该化合物能够结合到狒狒的C3上,并抵抗狒狒血液中的蛋白质水解裂解(与人类相似)。Compstatin TFA专一性地抑制灵长类动物的补体系统激活。其对补体经典途径和旁路途径的IC50值分别为63μM和12μM。
T77219 N-((Allyloxy)carbonyl)-N-methyl-L-alanine

N-((Allyloxy)carbonyl)-N-methyl-L-alanine 是一种丙氨酸衍生物。N-((Allyloxy)carbonyl)-N-methyl-L-alanine 可用于合成补体因子 D (complementfactor D) 抑制剂。补体因子 D 抑制剂可用于免疫系统相关疾病的研究。
T77089 Mirococept

Mirococept (APT070) 是一种抗体,靶向补体系统 (complement system) 的 C3b/C4b,也是一种膜定位的 C3转化酶抑制剂。Mirococept 减少 C 肽和促炎细胞因子的释放,并减少炎症细胞的浸润。Mirococept 减少胰岛内炎症,有利于胰岛移植。Mirococept 还抑制增加的肠和肺血管通透性以减少中性粒细胞流入。
T64692 AMY-101 acetate

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...

化合物

Complement factor D-IN-2
Cat.No: T38332
Synonym:
Target: Complement System
Compstatin
Cat.No: TP1304
Synonym: 坎普他汀
Target: Complement System
Eculizumab
Cat.No: T9915
Synonym:
Target: Complement System
Danicopan
Cat.No: T8509
Synonym: ACH-4471
Target: Complement System
Iptacopan hydrochloride
Cat.No: T9189
Synonym: Iptacopan HCl,LNP023 hydrochloride
Target: Complement System
JR14a
Cat.No: T9316
Synonym: 5-(Bis(4-chlorophenyl)methyl)-3-methylthiophene-2-carbonyl)-l-arginine hydrochloride
Target: Complement System
SB290157 trifluoroacetate
Cat.No: T12851
Synonym:
Target: Complement System
Leukadherin-1
Cat.No: T3638
Synonym:
Target: Integrin, Complement System
W-54011
Cat.No: T17250
Synonym:
Target: ROS, Complement System
ADH-503
Cat.No: T7776
Synonym: GB1275
Target: Complement System
Dexamethasone
Cat.No: T1076
Synonym: MK 125,Prednisolone F,NSC 34521,Hexadecadrol,地塞米松
Target: Glucocorticoid Receptor, Mitophagy, IL Receptor, SARS-CoV, Antibacterial, Antibiotic, Autophagy, Complement System
C3a (70-77)
Cat.No: T7497
Synonym: Complement 3a (70-77),C3a 70-77
Target: Complement System
(Z)-Leukadherin-1
Cat.No: T13379
Synonym: ADH-503 free base
Target: Complement System
C3a Receptor Agonist
Cat.No: T38287
Synonym: C3a receptor agonist 1,C3a受体激动剂,Complement 3a Receptor Agonist
Target: Complement System
Isatuximab
Cat.No: T38951
Synonym: SAR-650984,hu38SB19,Isatuximab-irfc
Target: Apoptosis, CD38
FD-IN-1
Cat.No: T11269
Synonym:
Target: Others
β-Amyloid (1-11)
Cat.No: TP1866
Synonym: β-amyloid 1-11
Target:
Compstatin TFA
Cat.No: T75775
Synonym:
Target:
N-((Allyloxy)carbonyl)-N-methyl-L-alanine
Cat.No: T77219
Synonym:
Target:
Mirococept
Cat.No: T77089
Synonym:
Target:
AMY-101 acetate
Cat.No: T64692
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T0945 Cyclosporin A

环孢素,Cyclosporine A,Ciclosporin,Cyclosporine,环孢菌素

Phosphatase; Antibiotic; Complement System Immunology/Inflammation; Metabolism; Microbiology/Virology
Cyclosporin A 属于天然产物,是一种真菌的活性代谢产物,一种环状多肽。Cyclosporin A 是一种能与亲环素结合的免疫抑制剂,可以抑制 calcineurin (IC50=7 nM)。
T40646 Lipoteichoic acid

Complement System Immunology/Inflammation
Lipoteichoic acid 是 Staphylococcus aureus 细胞壁的聚合物,通过诱导 C3 和抑制 CD55 来激活补体系统,通过 IGF-1 途径减少脂肪沉积。
TN3430 Apigenin 4'-O-rhamnoside

Others Others
Apigenin-4'-O-rhamnosylglucoside can strongly inhibit the classical pathway of the complement system.

天然产物

Cyclosporin A
Cat.No: T0945
Synonym: 环孢素,Cyclosporine A,Ciclosporin,Cyclosporine,环孢菌素
Target: Phosphatase, Antibiotic, Complement System
Lipoteichoic acid
Cat.No: T40646
Synonym:
Target: Complement System
Apigenin 4'-O-rhamnoside
Cat.No: TN3430
Synonym:
Target: Others
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