AMY-101 TFA(Synonyms: Cp40 TFA)

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AMY-101 TFA;(Synonyms: Cp40 TFA) 纯度: 99.94%

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。

AMY-101 TFAamp;;(Synonyms: Cp40 TFA)

AMY-101 TFA Chemical Structure

CAS No. : 1789738-04-0

规格 价格 是否有货 数量
1 mg ￥4000 In-stock
5 mg ￥9800 In-stock
10 mg ￥16500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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AMY-101 TFA 相关产品

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  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Macrocyclic Compound Library
  • Peptide Library

生物活性

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].

IC50 Target

KD: 0.5 nM (C3)[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

Formula

C83H117N23O18S2.xC2HF3O2
CAS 号

1789738-04-0
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 -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;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)
参考文献

  • [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.

    [3]. Yanyan Liu, et al. Complement C3 Produced by Macrophages Promotes Renal Fibrosis via IL-17A Secretion. Front Immunol. 2018 Oct 22;9:2385.