PPADS tetrasodium

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PPADS tetrasodiuma 是一种非选择性 P2X 受体拮抗剂。PPADS tetrasodiuma 阻断重组P2X1、-2、-3、-5，IC50 范围为1～2.6 μM。PPADS-tetrasodiuma 阻断天然 P2Y2 样 (IC50~0.9 mM) 和重组 P2Y4 (IC50~15 mM) 受体。PPADS tetrasodiuma 是豚鼠气道平滑肌 Na/Ca2? 交换逆模式的抑制剂。

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.

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.

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 hours for 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.

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Membrane Transporter/Ion Channel

P2X Receptor

P2X Receptor | Na+/Ca2+ Exchanger

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192575-19-2

599.3

C14H10N3Na4O12PS2

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : 50 mg/mL (83.43 mM; 超声助溶)

O=CC1=C(C(C)=NC(N=NC2=CC=C(S(=O)([O-])=O)C=C2S(=O)([O-])=O)=C1COP([O-])([O-])=O)O.[Na+].[Na+].[Na+].[Na+]

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(-20℃)

With Ice Pack

≥ 2 years