| Bioactivity | (D)-PPA 1 TFA is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 TFA serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 TFA binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy[1]. | ||||||
| Invitro | (D)-PPA 1 TFA (0.2 mg/mL, 1.0 mg/mL) 在 1.0 mg/mL 时阻断 PD-1/PD-L1 之间的相互作用[1]。(d) -ppa 1 (3.125-100 μM;24 h, 48 h) 不直接杀死肿瘤细胞，对 CT26 细胞生长无影响[1]。 | ||||||
| In Vivo | (D)-PPA 1 TFA (2 mg/kg; 皮下注射或腹腔注射; 每天 1 次, 共 7 天) 抑制小鼠体内 CT26 肿瘤的生长[1]。(D)-PPA 1 TFA (40 μg/mouse in 200 μL; i.v.; single dose) 具有靶向 CT26 荷瘤小鼠肿瘤组织的能力[1]。 | ||||||
| Name | (D)-PPA 1 TFA | ||||||
| Sequence | D-{Asn-Tyr-Ser-Lys-Pro-Thr-Asp-Arg-Gln-Tyr-His-Phe} | ||||||
| Shortening | D-{NYSKPTDRQYHF} | ||||||
| Formula | C72H99F3N20O23 | ||||||
| Molar Mass | 1669.67 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture and light, under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
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| Reference | [1]. Chang HN, et al. Blocking of the PD-1/PD-L1 Interaction by a D-Peptide Antagonist for Cancer Immunotherapy. Angew Chem Int Ed Engl. 2015 Sep 28;54(40):11760-4. |