AMY-101 (Cp40) 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 (Cp40) 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 (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[1][2].
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IC50 Target |
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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. |
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| Clinical Trial |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| Sequence Shortening |
YICV-{Trp(Me)}-QDW-{Sar}-AHRC-{N(Me)Ile}-NH2 (Disulfide bridge:Cys3-Cys13)
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| Solvent Solubility |
In Vitro:;
H2O
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:
| ; |
Contents |
Assign value |
| Acidic amino acid |
Asp (D), Glu (E), and the C-terminal -COOH. |
-1 |
| Basic amino acid |
Arg (R), Lys (K), His (H), and the N-terminal -NH2 |
+1 |
| 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) |
0 |
3.;;Recommended solution:
| Overall charge of peptide |
Details |
| Negative (lt;0) |
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. |
| Positive (gt;0) |
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. |
| Zero (=0) |
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. |
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| 参考文献 |
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[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.
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