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编 号：F755725
分子式：C27H25ClN4O3
分子量：488.97
分子式：C27H25ClN4O3
分子量：488.97
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CAS No: 2764596-06-5
产品详情
生物活性：
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel).
体内研究：
P-gp/BCRP-IN-1 (compound 19) (Male SD rats; 5 mg/kg PTX (IV), 20 mg/kg PTX (PO), 20 mg/kg PTX and 10 mg/kg compound 19 (PO); once) increases the bioavailability of PTX when PTX is given orally. Pharmacokinetic Parameters of P-gp/BCRP-IN-1 in male SD rats.PTX (5 mg/kg) PTX (20 mg/kg) PTX (20 mg/kg) with 19 (10 mg/kg)
Routemax (h)IVPOPO
AUC0-t (ng*h/mL)1734.95 ± 244.28610.89 ± 45.623131.51 ± 63.17
Cmax (ng/mL)925.86 ± 31.39112.09 ± 25.46652.31 ± 41.93
Tmax (h)0.44 ± 0.052.00 ± 0.032.51 ± 0.19
T1/2 (h)0.12 ± 0.031.35 ± 0.051.68 ± 0.15
Vd/F (L)5.06 ± 0.0967.38 ± 12.5416.04 ± 0.08
CL/F (L/h)2.88 ± 0.1432.74 ± 5.426.18 ± 0.36
F (%)1008.8045.1
Animal Model:Male SD rats (n = 15, three groups)
Dosage:5 mg/kg PTX (IV); 20 mg/kg PTX (PO); 20 mg/kg PTX with 10 mg/kg compound 19 (PO)
Administration:IV, PO, once (Pharmacokinetic Analysis)
Result:Increased the bioavailability of PTX when PTX was given orally.
体外研究：
P-gp/BCRP-IN-1 (compound 19) (0-200 μM, 48 h) has a weak anti-proliferative activity against A549 cells, and shows low cytotoxicity to the K562 , K562/A02, MDCK-II, MDCK-II-BCRP cells.P-gp/BCRP-IN-1 (48 h) exhibits the great reversal effect of resistance to both ADM (Adriamycin) and MX (Mitoxantrone) in K562/A02 cells and MDCK-II-BCRP cells, and increases the reversal activity of ADM (0-5 μM) and MX (0-20 μM) in a concentration-dependent manner.P-gp/BCRP-IN-1 (0-5 μM, 4 h) increases drug accumulation and prevents efflux of P-gp and BCRP. P-gp/BCRP-IN-1 (0-5 μM, 48 h) dose not affect the expression of P-gp as well as BCRP protein.P-gp/BCRP-IN-1 (0-200 μM, 4 h) decreases the viability of Caco-2 cells, inhibits the intestinal P-gp-mediated efflux of PTX and increases its concentration in the intestinal cells, can enhance the absorption and bioavailability.P-gp/BCRP-IN-1 prevents intracellular accumulation of anti-neoplastic drugs by impairing the function of P-gp and BCRP.
P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel).
体内研究：
P-gp/BCRP-IN-1 (compound 19) (Male SD rats; 5 mg/kg PTX (IV), 20 mg/kg PTX (PO), 20 mg/kg PTX and 10 mg/kg compound 19 (PO); once) increases the bioavailability of PTX when PTX is given orally. Pharmacokinetic Parameters of P-gp/BCRP-IN-1 in male SD rats.PTX (5 mg/kg) PTX (20 mg/kg) PTX (20 mg/kg) with 19 (10 mg/kg)
Routemax (h)IVPOPO
AUC0-t (ng*h/mL)1734.95 ± 244.28610.89 ± 45.623131.51 ± 63.17
Cmax (ng/mL)925.86 ± 31.39112.09 ± 25.46652.31 ± 41.93
Tmax (h)0.44 ± 0.052.00 ± 0.032.51 ± 0.19
T1/2 (h)0.12 ± 0.031.35 ± 0.051.68 ± 0.15
Vd/F (L)5.06 ± 0.0967.38 ± 12.5416.04 ± 0.08
CL/F (L/h)2.88 ± 0.1432.74 ± 5.426.18 ± 0.36
F (%)1008.8045.1
Animal Model:Male SD rats (n = 15, three groups)
Dosage:5 mg/kg PTX (IV); 20 mg/kg PTX (PO); 20 mg/kg PTX with 10 mg/kg compound 19 (PO)
Administration:IV, PO, once (Pharmacokinetic Analysis)
Result:Increased the bioavailability of PTX when PTX was given orally.
体外研究：
P-gp/BCRP-IN-1 (compound 19) (0-200 μM, 48 h) has a weak anti-proliferative activity against A549 cells, and shows low cytotoxicity to the K562 , K562/A02, MDCK-II, MDCK-II-BCRP cells.P-gp/BCRP-IN-1 (48 h) exhibits the great reversal effect of resistance to both ADM (Adriamycin) and MX (Mitoxantrone) in K562/A02 cells and MDCK-II-BCRP cells, and increases the reversal activity of ADM (0-5 μM) and MX (0-20 μM) in a concentration-dependent manner.P-gp/BCRP-IN-1 (0-5 μM, 4 h) increases drug accumulation and prevents efflux of P-gp and BCRP. P-gp/BCRP-IN-1 (0-5 μM, 48 h) dose not affect the expression of P-gp as well as BCRP protein.P-gp/BCRP-IN-1 (0-200 μM, 4 h) decreases the viability of Caco-2 cells, inhibits the intestinal P-gp-mediated efflux of PTX and increases its concentration in the intestinal cells, can enhance the absorption and bioavailability.P-gp/BCRP-IN-1 prevents intracellular accumulation of anti-neoplastic drugs by impairing the function of P-gp and BCRP.
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