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。
生物活性 | AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the centralcomplement componentC3(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 | |
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. |
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
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: DMSO : 100 mg/mL(54.08 mM;Need ultrasonic) H2O : 50 mg/mL(27.04 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 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本网站选购。
|