产品
编 号:F753893
分子式:C37H60N14O14S2
分子量:989.09
产品类型
结构图
CAS No: 2580154-02-3
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产品详情
生物活性:
Certepetide (CEND-1) is a bifunctional cyclic peptide (a.k.a. iRGD). Certepetide is a tumor-penetrating enhancer via RGD motif interaction with alphav-integrins and via activating NRP-1, and transforms the solid tumor microenvironment into a temporary agent conduit. Certepetide accumulates in tumors, and is used in the research of pancreatic cancer and other solid tumors.
体内研究:
CEND-1 (iRGD) 可以调节固体肿瘤微环境,增强共同给药的抗癌药物的输送和治疗指数.CEND-1可以增强抗癌治疗药物特异性地渗透到肿瘤中,而不是正常组织,同时还有减少剂量的潜力,可以减轻副作用.CEND-1 (静脉注射) 会将联合给药的伊万斯蓝的效果提高约三倍. Table 1. Derived mean pharmacokinetic parameters for CEND-1 in mouse, rat, dog and monkey plasma after a single intravenous infusion of CEND-1 (±SD) . Number of Animals (Sex)CEND-1 Dose (mg/kg)t1/2 (h)C0 (ng/mL)V (mL/kg)Cl_obs (mL/hr/kg)AUC0-inf (h*ng/mL)
Mouse *
3 (M)1.50.30610,34344910161476
3 (M)13.50.54768,3581007127710,569
Rat*
6 (M)750.341469,000171348215,476
6 (F)750.391436,333254451166,331
Dog*
3 (M)10.665 (0.0448) 6010 (1985)241 (27)253 (40.1)4030 (686)
3 (F)50.648 (0.0486) 25,133 (3635)230 (14.6)247 (32.9)20,443 (2530)
Monkey*
3 (M)50.888 (0.0963) 55,082 (19,905)204 (14.1)179 (23.4)28,230 (3865)
3 (M)500.956 (0.0869) 602,161 (211,386)162 (32.1)178 (51.9)421,119 (171,418)
Note:* Because of volume limitations in the mice and rats, each animal was used for one time point sampling, limiting the statistical analysis of the data. M, male; F, female.