产品
编 号:F239599
分子式:C14H10N3Na4O12PS2
分子量:599.3
产品类型
结构图
CAS No: 192575-19-2
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产品详情
生物活性:
PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca2+ exchanger in guinea pig airway smooth muscle.
体内研究:
PPADS tetrasodiuma (15-60 mg/100g body weight (BW); i.p.; every 12 hoursfor 8 days) inhibits glomerular mesangial cells (MC) proliferation without altering proliferation of non-MC in vivo in mesangial proliferative glomerulonephritis.Animal Model:Male Sprague-Dawley ratsweighing 160 to 200 g (anti-Thy1 disease mode)
Dosage:15 mg/100g BW, 30 mg/100g BW, 60 mg/100g BW
Administration:i.p.; every 12 hoursfor 8 days (the first PPADS injection was administered 60 minutes after disease induction, and the loading dose always contained double the amount of PPADS compared to the following injections.)
Result:Specifically and dose-dependently reduced early (day 3) glomerular mesangial cell proliferation without altering proliferation of non-MC.
体外研究:
PPADS tetrasodiuma (1-30 μM; 10-50 minutes) inhibits Na+/Ca2+ exchanger reverse mode (NCXREV) in a time- and concentration dependent manner.PPADS tetrasodiuma is effective at other native and recombinant P2XRs. At human P2XRs sensitivity to PPADS tetrasodiuma depended on the subtype and is highest at the hP2X1, -2, -3, -5, and -7Rs with an IC50 of ~1-3 and ~30 μM for the hP2X4R.