磷酸乙二醛-6-偶氮苯基-2'，4'-二磺酸四钠盐 | 192575-19-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 磷酸乙二醛-6-偶氮苯基-2'，4'-二磺酸四钠盐
• 中文别名: 磷酸吡哆醛-6-偶氮(苯-2,4-二磺酸)四钠盐水合物
• 英文名称: Ppads tetrasodium salt
• 英文别名: tetrasodium;4-[[4-formyl-5-hydroxy-6-methyl-3-(phosphonatooxymethyl)pyridin-2-yl]diazenyl]benzene-1,3-disulfonate
• CAS: 192575-19-2
• 化学式: C14H10N3Na4O12PS2
• 分子量: 599.3
• InChiKey: KURWUCJJNVPCHT-UHFFFAOYSA-J

物化性质

• 溶解度：
  H2O: >10 mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  -12.51
• 重原子数：
  36
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  279
• 氢给体数：
  1
• 氢受体数：
  15

制备方法与用途

生物活性

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。

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 was highest at the hP2X1, -2, -3, -5, and -7Rs with an IC50 of ∼1–3 and ∼30 μM for the hP2X4R.

体内研究

PPADS tetrasodiuma (15-60 mg/100g body weight (BW); i.p.; every 12 hours for 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.