AMY-101 (Cp40), 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.
KD: 0.5 nM (C3).
体内研究 (In Vivo)
AMY-101 can improve the periodontal condition of NHPs with natural chronic periodontitis. AMY-101 can induce a long-lasting anti-inflammatory effect. 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. 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.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Fifteen adult male cynomolgus monkeys (Macaca fascicularis) (7-15 years old; 5.0-7.6 kg body weight).
0.1 mg/site; 50 μL of 2 mg/mL solution.
Injected locally. (Either three times per week or once a week for 6 weeks followed by a 6-week follow-up period without treatment.)
Does not cause irritation in healthy gingiva.
UUO and sham-operated mice.
Subcutaneous injection every 12 h, daily, 7 or 14 days.
1 mg/kg Cp40 had much less severe interstitial fibrosis than control peptide-injected mice.
Room temperature in continental US; may vary elsewhere.
Please store the product under the recommended conditions in the Certificate of Analysis.
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
Overall charge of peptide
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
. 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.
. Mastaglio S, et al. The first case of COVID-19 treated with the complement C3 inhibitor AMY-101. Clin Immunol. 2020 Apr 29:108450
. Yanyan Liu, et al. Complement C3 Produced by Macrophages Promotes Renal Fibrosis via IL-17A Secretion. Front Immunol. 2018 Oct 22;9:2385.