AMY-101 acetate(Synonyms: Cp40 acetate)

发表于由

AMY-101 acetate;(Synonyms: Cp40 acetate) 纯度: 99.93%

AMY-101 acetate (Cp40 acetate) 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 acetate (Cp40 acetate) 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 acetateamp;;(Synonyms: Cp40 acetate)

AMY-101 acetate Chemical Structure

规格 价格 是否有货 数量
1 mg ￥3700 In-stock
5 mg ￥9100 In-stock
10 mg ￥15300 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

* Please select Quantity before adding items.

AMY-101 acetate 相关产品

bull;相关化合物库:

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

生物活性

AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) 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

分子量

1849.16

Formula

C85H121N23O20S2
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:;

DMSO : 100 mg/mL (54.08 mM; Need ultrasonic)

H2O : 50 mg/mL (27.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.5408 mL 2.7039 mL 5.4079 mL
5 mM 0.1082 mL 0.5408 mL 1.0816 mL
10 mM 0.0541 mL 0.2704 mL 0.5408 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: ≥ 2.5 mg/mL (1.35 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.35 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (1.35 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (1.35 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.35 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.35 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
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]. 1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice.