AMY-101 TFA (Cp40 TFA) 是补体 C3 的肽类抑制剂 (KD= 0.5 nM),可抑制非人类灵长类动物自然发生的牙周炎。AMY-101 TFA (Cp40 TFA) 在 COVID-19 重症肺炎合并全身超炎症模型中具有良好的抗炎活性。
生物活性 | AMY-101 TFA (Cp40 TFA), a peptidic inhibitor of the centralcomplement componentC3(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]. |
IC50& Target | |
体内研究 (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]. AMY-101 (Cp40, 1 mg/kg, sc, injection every 12 h, daily, 7 or 14 days) attenuates fibrosis and infiltration of inflammatory cells in UUO-induced renal fibrosis[3].
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. |
Animal Model: | UUO and sham-operated mice[3]. | Dosage: | 1 mg/kg. | Administration: | Subcutaneous injection every 12 h, daily, 7 or 14 days. | Result: | 1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice. |
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Clinical Trial | |
性状 | |
Formula | |
CAS 号 | |
Sequence Shortening | YICV-{Trp(Me)}-QDW-{Sar}-AHRC-{N(Me)Ile}-NH2 (Disulfide bridge:Cys3-Cys13) |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Sealed storage, away from moisture and light Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: H2O : 100 mg/mL(Need ultrasonic) DMSO : 100 mg/mL(Need ultrasonic) |