| Identification | Back Directory | [Name]
(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-5-(diaminomethylideneamino)pen tanoyl]amino]hexanoyl]amino]hexanoyl]amino]-N-[(1R)-1-[[(1R)-1-[[(1R)- 1-[[(1R)-1-[[(1R)-1-carbamoyl-2-(4-hydroxyphenyl)ethyl]carbamoylmethyl carbamoyl]pentyl]carbamoyl]pentyl]carbamoyl]pentyl]carbamoyl]-4-(diami nomethylideneamino)butyl]hexanamide | [CAS]
287096-87-1 | [Synonyms]
RDP5 RDP-5 RDP1258 RDP-1258 Delmitide Allotrap-1258 Rationally Designed Peptide-58 D-Tyrosinamide, D-arginyl-D-norleucyl-D-norleucyl-D-norleucyl-D-arginyl-D-norleucyl-D-norleucyl-D-norleucylglycyl- (2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-aMino-5-(diaMinoMethylideneaMino)pen tanoyl]aMino]hexanoyl]aMino]hexanoyl]aMino]-N-[(1R)-1-[[(1R)-1-[[(1R)- 1-[[(1R)-1-[[(1R)-1-carbaMoyl-2-(4-hydroxyphenyl)ethyl]carbaMoylMethyl carbaMoyl]pentyl]carbaMoyl]pentyl]carbaMoy (2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-5-(diaminomethylideneamino)pen tanoyl]amino]hexanoyl]amino]hexanoyl]amino]-N-[(1R)-1-[[(1R)-1-[[(1R)- 1-[[(1R)-1-[[(1R)-1-carbamoyl-2-(4-hydroxyphenyl)ethyl]carbamoylmethyl carbamoyl]pentyl]carbamoyl]pentyl]carbamoyl]pentyl]carbamoyl]-4-(diami nomethylideneamino)butyl]hexanamide | [Molecular Formula]
C59H105N17O11 | [MOL File]
287096-87-1.mol | [Molecular Weight]
1228.57 |
| Hazard Information | Back Directory | [Uses]
Treatment of chemotherapy-induced diarrhea. | [in vivo]
Delmitide (oral; 2.5, 5, 10 mg/kg; daily) significantly reduced CPT-11induced diarrhea, mucosal inflammation, and mortality in mice by suppressing the overproduction of proinflammatory cytokines TNF-a, IFN-y, and IL-12 in vivo[2].
Delmitide (oral; 2.5, 5, 10 mg/kg; daily) generates an enhanced tumor response and prolongation of time to relapse without concomitant Gl toxicity in mice[2]. | Animal Model: | BALB/c mice (female, 9-10-week)[2] | | Dosage: | 2.5, 5, 10 mg/kg or 0.2 mL, 10 mg/kg | | Administration: | Oral, daily | | Result: | Reduced the incidence of diarrhea and attenuated CPT-11-associated GI toxicity and mortality in a dose-dependent manner.
Had protective effect against chemotherapy-induced GI side-effects and reduced CPT-11-induced overexpression of TNF-α, IFN-γ, and IL-12 in vivo.
Preserved the intestinal mucosa morphology by maintaining villus and crypt structure and inhibited TNF-α-mediated apoptosis in the crypt compartment, thereby protecting intestinal mucosa integrity in mice.
Protected mice from CPT-11-induced GI toxicity and mortality and enhanced animal survival in tumor-bearing mice.
Significantly reduced the incidence and overall tumor burden in a spontaneously metastatic model.
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Fuan Bio
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