Vipivotide tetraxetan (PSMA-617) 是一种化学修饰的 PSMA(prostate-specific membrane antigen) 抑制剂，Ki值为0.37 nM。 Information Vipivotide tetraxetan (PSMA-617) is a chemically modified PSMA(prostate-specific membrane antigen) inhibitor with a Ki of 0.37 nM. Targets PSMA (Cell-free assay) 0.37 nM(Ki) In vitro PSMA-617 demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant Ki = 2.34 ± 2.94 nM on LNCaP; Ki = 0.37 ± 0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated. In vivo The small-animal PET measurements show high tumor-to-background contrasts as early as 1 h after injection. In vivo distribution reveals specific uptake in LNCaP tumors and in the kidneys 1 h after injection. With regard to therapeutic use, PSMA-617 exhibits a rapid clearance from the kidneys from 113.3 ± 24.4 at 1 h to 2.13 ± 1.36 percentage injected dose per gram at 24 h. The favorable pharmacokinetics of the molecule leads to tumor-to-background ratios of 1,058 (tumor to blood) and 529 (tumor to muscle), respectively,24 h after injection. Cell Research(from reference) Cell lines：PSMA-positive LNCaP cell line Concentrations：0–5000 nM Incubation Time：1 h
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Vipivotide tetraxetan (PSMA-617)
CAS number：1702967-37-0 molecular formula：C49H71N9O16
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| Chinese alias | Vipivotide 四西坦 (PSMA-617) | ||
| English alias | 1702967-37-0 | Vipivotide tetraxetan | s8670 | PSMA617 | PSMA-617 | Sodium phosphate monobasic monohydrate, BioXtra, for molecular biology, >=99.5% (T) | NACLO3 | -LYSINE, N2-((((1S)-1,3-DICARBOXYPROPYL)AMINO)CARBONYL)-N6-(3-(2-NAPHTHALENYL)-N-((TRANS-4-( | ||
| CAS number | 1702967-37-0 | molecular formula | C49H71N9O16 |
| molecular weight | 1042.14 g/mol | Exact mass | - |
| PSA | 365.000 Ų | logp | -11.549 |
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