AMY-101 TFA

Names

[ CAS No. ]:
1789738-04-0

[ Name ]:
AMY-101 TFA

Biological Activity

[Description]:

AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> SARS-CoV
Signaling Pathways >> Immunology/Inflammation >> Complement System
Research Areas >> Inflammation/Immunology

[Target]

KD: 0.5 nM (C3)[1].


[In Vivo]

AMY-101 can improve the periodontal condition of NHPs with natural chronic periodontitis[1]. AMY-101 can induce a long-lasting anti-inflammatory effect[1]. AMY-101 (4 mg/kg bodyweight, subcutaneous injection. once per 24 hr for a total of 28 days) causes a significant and long-lasting reduction in PPD, an index that measures tissue destruction[1]. Animal Model: Fifteen adult male cynomolgus monkeys (Macaca fascicularis) (7 – 15 years old; 5.0 – 7.6 kg body weight)[1]. Dosage: 0.1 mg/site; 50 μL of 2 mg/mL solution. Administration: Injected locally. (Either three times per week or once a week for 6 weeks followed by a 6-week follow-up period without treatment.) Result: Does not cause irritation in healthy gingiva.

[References]

[1]. Kajikawa T, et al. Safety and Efficacy of the Complement Inhibitor AMY-101 in a Natural Model of Periodontitis in Non-human Primates. Mol Ther Methods Clin Dev. 2017 Aug 18;6:207-215.

[2]. Mastaglio S, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101. Clin Immunol. 2020 Apr 29:108450.

Chemical & Physical Properties

[ Molecular Formula ]:
C83H117N23O18S2.xC2HF3O2


Related Compounds