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编 号:F306080
分子式:C59H105N17O11
分子量:1228.57
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Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis.

体内研究:
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.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.Animal Model:BALB/c mice (female, 9-10-week)
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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