ChemicalBook CAS DataBase List 1789738-04-0

1789738-04-0

Name	Cp40 TFA
CAS	1789738-04-0
Molecular Formula	C85H118F3N23O20S2
Molecular Weight	1903.14
MOL File	1789738-04-0.mol

Chemical Properties

form	Solid
color	White to off-white
Sequence	{D-Tyr}-Ile-Cys-Val-{Trp(Me)}-Gln-Asp-Trp-{Sar}-Ala-His-Arg-Cys-{N(Me)Ile}-NH2 (Disulfide bridge:Cys3-Cys13)

Hazard Information

Uses

AMY-101 TFA (Cp40 TFA), 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].

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.

References

[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. DOI:10.1016/j.omtm.2017.08.001
[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. DOI:10.1016/j.clim.2020.108450
[3] Yanyan Liu, et al. Complement C3 Produced by Macrophages Promotes Renal Fibrosis via IL-17A Secretion. Front Immunol. 2018 Oct 22;9:2385. DOI:10.3389/fimmu.2018.02385

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