Rostafuroxin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rostafuroxin (PST2238) 是一种有效的、选择性的、口服活性的 Na-K-ATPase 抑制剂，可取代狗肾 Na+,K+-ATPase 中的 3H 哇巴因，IC50 为 1.5 nM。

Rostafuroxin (PST2238) is potent, selective, orally active Na-K-ATPase inhibitor, displaces 3H ouabain from dog kidney Na+,K+-ATPase with IC50 of 1.5 nM; displays excellent selectivity over a panel of general and hormonal receptors, with exception of thromboxane A2 receptor (61% inhibition at 1 uM); abolishes ouabain-dependent increase in the Na-K pump rate in cultured renal cells, abolishes the increase in blood pressure and renal Na-K ATPase activity caused by ouabain in rats model of hypertension.Hypertension Phase 2 Clinical(In Vitro):Rostafuroxin (PST 2238) competitively inhibits Ouabain (HY-B0542) binding and signaling. Rostafuroxin antagonizes the molecularand functional effects of Ouabain by reversing the ouabain-induced, Src-dependent Na+,K+-ATPase phosphorylation and activation.Rostafuroxin (0.125-128 μM; for 24 h post treatment) has less than 20% reduction in cell viability in A549 cells and HSAEC. Rostafuroxin inhibits the expression of RSV-GFP in HSAEC (IC50=1.8 μM) and A549 cells (IC50=14.8 μM).Rostafuroxin displaced [3H]Ouabain from the dog kidney Na+,K+-ATPase receptor (IC50=1.5 nM), is devoid of cardiac inotropic activity in isolated guinea pig atria, and shows no affinity up to 10-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate,glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors.(In Vivo):Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation.

Rostafuroxin (PST 2238) competitively inhibits Ouabain (HY-B0542) binding and signaling. Rostafuroxin antagonizes the molecularand functional effects of Ouabain by reversing the ouabain-induced, Src-dependent Na+,K+-ATPase phosphorylation and activation. Rostafuroxin (0.125-128 μM; for 24 h post treatment) has less than 20% reduction in cell viability in A549 cells and HSAEC. Rostafuroxin inhibits the expression of RSV-GFP in HSAEC (IC50=1.8 μM) and A549 cells (IC50=14.8 μM). Rostafuroxin displaced [3H]Ouabain from the dog kidney Na+,K+-ATPase receptor (IC50=1.5 nM), is devoid of cardiac inotropic activity in isolated guinea pig atria, and shows no affinity up to 10-4 M with general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutammate,glycine, benzodiazepine) and hormonal (estrogenic, progestinic, androgenic, mineralcorticoid) receptors.

Rostafuroxin (PST 2238; 1 mg/kg/day; gavage; for 3 weeks) decreases SBP and improves acetylcholine-induced relaxation. Animal Model:Male 7-week-old Wistar ratsDosage:1 mg/kg Administration:Gavage; daily; for 3 weeks Result:Decreased SBP, improved acetylcholine-induced relaxation via enhanced nitric oxide synthesis and bioavailability, decreased superoxide anion generation from NAD(P)H oxidase and cyclooxygenase-2 and reduced cytoplasmic tyrosine kinase Src phosphorylation.

PST-2238 | PST2238 | PST 2238

Membrane Transporter/Ion Channel

Na-K-ATPase

Na+/K+-ATPase

Cardiovascular Disease

Hypertension

156722-18-8

374.5137

C23H34O4

>98% (HPLC)

10 mM in DMSO

C[C@@]12[C@](C3=COC=C3)(O)CC[C@]1(O)[C@]4([H])CC[C@]5([H])C[C@@H](O)CC[C@]5(C)[C@@]4([H])CC2

24-Norchola-20,22-diene-3,14,17-triol, 21,23-epoxy-, (3β,5β,14β)-

(-20℃)

With Ice Pack

≥ 2 years