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 centralcomplement componentC3(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]. |
| 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. |
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| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| 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 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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 (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>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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