AMY-101
(Synonyms: Cp40) 目录号 : GC39697
AMY-101（Cp40）是一种高效的中枢补体成分C3抑制剂，对C3具有亚纳摩尔级亲和力（KD=0.5nmol/L）。
Cas No.:1427001-89-5
Sample solution is provided at 25 µL, 10mM.
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AMY-101 (Cp40) is the efficient inhibitor of the central complement component C3, with sub-nanomolar affinity for C3 (KD=0.5nmol/L)[1]. AMY-101 is involved in regulating the immune response, regulating the complement system and the release of inflammatory mediators[2]. AMY-101 has been used in immune response research, anti-inflammatory experiments and antiviral study[3].
In vitro, AMY-101 treatment (20μmol/L) for 72 hours significantly reduced the production of pro-inflammatory mediators in human THP-1 cells[4]. Treatment of SV40-immortalized porcine aortic endothelial cells with AMY-101 at 20μg/ml for 1 hour almost completely inhibited the deposition of C3 fragments and C5b-9 on the cells[5].
In vivo, AMY-101 treatment (4mg/kg; 28 days) via subcutaneous injection daily to adult cynomolgus monkeys can significantly reduce the clinical indices measured for periodontal inflammation and tissue destruction[1]. In sensitized male rhesus monkeys, intramuscular injection of AMY-101 (2mg/kg/day; I.M.) for 16 days can inhibit lymphocyte activation and proliferation, prevent antibody-mediated rejection reactions, and prolong the survival period of kidney transplantation[6].
References:
[1] Kajikawa T, Briones R A, Resuello R R G, et al. Safety and efficacy of the complement inhibitor AMY-101 in a natural model of periodontitis in non-human primates[J]. Molecular Therapy Methods & Clinical Development, 2017, 6: 207-215.
[2] Li J, Xu Z, Ayre W N, et al. AMY-101 as complement C3 inhibitor for periodontitis therapy: mechanisms, efficacy, and clinical translation[J]. Frontiers in Immunology, 2025, 16: 1587126.
[3] Mastaglio S, Ruggeri A, Risitano A M, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101[J]. Clinical immunology, 2020, 215: 108450.
[4] Fernandes D C, Silva-de-França F, Pohl P C, et al. Cp40-mediated complement C3 inhibition dampens inflammasome activation and inflammatory mediators storm induced by Bitis arietans venom[J]. International Immunopharmacology, 2025, 147: 113701.
[5] Wang J, Wang L, Xiang Y, et al. Using an in vitro xenoantibody-mediated complement-dependent cytotoxicity model to evaluate the complement inhibitory activity of the peptidic C3 inhibitor Cp40[J]. Clinical Immunology, 2016, 162: 37-44.
[6] Schmitz R, Fitch Z W, Schroder P M, et al. C3 complement inhibition prevents antibody-mediated rejection and prolongs renal allograft survival in sensitized non-human primates[J]. Nature Communications, 2021, 12(1): 5456.
AMY-101（Cp40）是一种高效的中枢补体成分C3抑制剂，对C3具有亚纳摩尔级亲和力（KD=0.5nmol/L）[1]。AMY-101通过调控补体系统和炎症介质释放参与免疫反应调节[2]。AMY-101已应用于免疫应答研究、抗炎实验及抗病毒研究[3]。
在体外，20μmol/L浓度的AMY-101处理人THP-1细胞72小时后，能显著降低促炎介质的产生[4]。使用20μg/ml剂量的AMY-101处理SV40永生化猪主动脉内皮细胞1小时，几乎完全抑制了细胞表面C3片段和C5b-9的沉积[5]。
在体外，成年食蟹猴每日皮下注射4mg/kg剂量的AMY-101持续28天，可显著改善牙周炎症和组织破坏的临床指标[1]。对致敏雄性恒河猴进行16天肌肉注射治疗（2mg/kg/day），能抑制淋巴细胞活化增殖，预防抗体介导的排斥反应，并延长肾移植后的存活期[6]。
| Cell experiment [1]: | |
Cell lines | THP-1 cells |
Preparation Method | THP-1 cells were seeded in 96-well plates at a density of 2.5 × 104cells per well with 200μL of complete RPMI 1640 medium that contained 50nmol/L Phorbol 12-Myristate 13-Acetate (PMA). The cells remained in incubation for 48 hours with an atmosphere of 5% CO2 at 37°C. The medium containing PMA was exchanged with complete RPMI(200μL/well) and cells rested for another 24 hours before treatment. The medium was switched to complete RPMI with 1%FBS two hours before treatment. The cells received a treatment with LPS at concentrations of 0.01 or 0.10μg/mL or Bitis arietans venom(BVA) at 5.0, 6.25, 12.5, 25.0, or 50.0μg/mL concentrations and saline as a negative control. After incubating the cells at 24, 48, and 72 hours the supernatants were collected and stored at −80°C for subsequent examination. The experimental cells received treatments with BVA at 50μg/mL concentration, AMY-101 at 20μmol/L concentration, and saline solution for periods of 24, 48, 72h. The MTT assay determined cell viability while the inflammatory cytokine kit measured cytokine levels. |
Reaction Conditions | 20μmol/L; 24, 48, 72h |
Applications | AMY-101 significantly reduced the level of IL-1β for 72 hours and had an inhibitory effect on the activation of inflammasomes. |
| Animal experiment [2]: | |
Animal models | Adult cynomolgus monkeys |
Preparation Method | The research utilized adult cynomolgus monkeys which ranged from 7 to 10 years old and weighed between 5.0 and 7.6 kilograms. After four weeks of program adaptation scientists used socially-placed monkeys in stainless steel cages for experiments. Research animals gain environmental richness from daily care by technicians and environment-rich items combined with visual contact with other animals. The research animals received specific quantities of authorized feed mixture as part of their diet. The animals had unrestricted access to fresh drinking water. Deliver AMY-101 subcutaneously at a rate of 4mg/kg/day for 28 days through a 1mL insulin-safe syringe fitted with a 28G×1/2-inch needle. Conduct clinical examinations initially at week 0 and then at each of the subsequent study intervals of weeks 1 through 4 and at week 11. Samples were collected from both gingiva and bone tissue at the beginning of the study and again at 4 and 11 weeks. |
Dosage form | 4mg/kg /day for 28 days; s.c. |
Applications | AMY-101 treatment significantly reduced the inflammatory clinical parameters of naturally occurring chronic periodontitis in adult cynomolgus monkeys. |
References: | |
| Cas No. | 1427001-89-5 | SDF | |
| 别名 | Cp40 | ||
| 分子式 | C83H117N23O18S2 | 分子量 | 1789.11 |
| 溶解度 | 100mg/mL in Water | 储存条件 | Store at -20°C, Protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.5589 mL | 2.7947 mL | 5.5894 mL |
| 5 mM | 0.1118 mL | 0.5589 mL | 1.1179 mL |
| 10 mM | 0.0559 mL | 0.2795 mL | 0.5589 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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