|2-((4R,7S,10S,13S,19S,22S,25S,28S,31S,34R)-10-((1H-咪唑-5-基)甲基)-19-((1H-吲哚-3-y基)甲基)-34-((2S,3S)-2-((R)-2-氨基-3-(4-羟基苯基)丙酰胺基)-3-甲基戊酰胺基)-4-(((2S,3S)-1-氨基-3-甲基-1-氧代戊-2-基)(甲基)氨基甲酰基)-25-(3-氨基-3-氧代丙基)-7-(3-胍基丙基)-31-异丙基-13,17-二甲基-28-((1-甲基-1H-吲哚-3-基)甲基)-6,9,12,15,18,21,24,27,30,33-十氧代-1,2-二硫杂-5,8,11,14,17,20,23,26,29,32-十氮杂环三十五烷-22-基)乙酸乙酸盐|CsnPharm

CAS No.: N/A

2-((4R,7S,10S,13S,19S,22S,25S,28S,31S,34R)-10-((1H-Imidazol-5-yl)methyl)-19-((1H-indol-3-yl)methyl)-34-((2S,3S)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-methylpentanamido)-4-(((2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl)(methyl)carbamoyl)-25-(3-amino-3-oxopropyl)-7-(3-guanidinopropyl)-31-isopropyl-13,17-dimethyl-28-((1-methyl-1H-indol-3-yl)methyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decaazacyclopentatriacontan-22-yl)acetic acid compound acetic acid salt Catalog No. CSN27744

Synonyms: AMY-101 acetate

AMY 101 is a peptidic central complement component C3 inhibitor with Kd value of 0.5nM. It is now in phase 2 study of Gingivitis, Periodontitis and SARS-CoV-2 acute respiratory disease.

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生物活性

描述Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses^[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute to the development of alcohol-induced fatty liver and its consequences^[4].AMY-101 TFA (Cp40 TFA) is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). It shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation^[5].a daily subcutaneous dose of AMY-101 (4 mg/kg bodyweight) was protective against NHP periodontitis, suggesting that patients treated for systemic disorders (e.g., paroxysmal nocturnal hemoglobinuria) can additionally benefit in terms of improved periodontal condition^[6].Plasma concentrations of both C3 and Cp40 were measured periodically and complete saturation of plasma C3 was confirmed. No differences in hematological, biochemical, or immunological parameters were identified in the blood or tissues of animals treated with Cp40 when compared to those injected with vehicle alone. Further, skin wounds showed no signs of infection in those treated with Cp40.Cp40 treatment was associated with a trend toward accelerated wound healing when compared with the control group. In addition, a biodistribution study in a rhesus monkey indicated that the distribution of Cp40 in the body is associated with the presence of C3, concentrating in organs that accumulate blood and produce C3^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.5408 mL
- 2.7040 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

技术信息

CAS号	N/A	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C85H121N23O20S2	运输	蓝冰
分子量	1849.14	别名	AMY-101 acetate

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