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287096-87-1

287096-87-1 Structure

287096-87-1 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.29±0.1 g/cm3(Predicted)
[pka]

9.87±0.15(Predicted)
[Sequence]

d(Arg-{Nle}-{Nle}-{Nle}-Arg-{Nle}-{Nle}-{Nle}-Gly-Tyr-NH2)
Hazard InformationBack 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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