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Beraprost sodium Sale

(Synonyms: (Rac)-贝拉前列素钠) 目录号 : GC38891

A stable, orally active analog of prostacyclin

Beraprost sodium Chemical Structure

Cas No.:496807-11-5

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10mM (in 1mL DMSO)
¥2,970.00
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5mg
¥2,700.00
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10mg
¥4,500.00
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25mg
¥8,550.00
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产品描述

Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 ?g in humans, given 1 to 3 times per day, have been demonstrated to improve clinical end points in diseases responsive to prostacyclin. Oral beraprost therapy improved the survival and pulmonary hemodynamics of patients with primary pulmonary hypertension.1 Beraprost inhibits platelet aggregation in healthy subjects and in diabetic patients at similar doses.2,3

1.Nagaya, N., Uematsu, M., Okano, Y., et al.Effect of orally active prostacyclin analogue on survival of outpatients with primary pulmonary hypertensionJ. Am. Coll. Cardiol.341188-1192(1999) 2.Nony, P., Ffrench, P., Girard, P., et al.Platelet-aggregation inhibition and hemodynamic effects of beraprost sodium, a new oral prostacyclin derivative: A study in healthy male subjectsCan. J. Physiol. Pharmacol.74887-893(1996) 3.Kato, H., Takashima, T., Kishikawa, H., et al.Effect of beraprost sodium, a stable prostaglandin I2 analogue, on platelet aggregation in diabetes mellitusInt. J. Clin. Pharmacol. Res.16(4-5)99-102(1996)

Chemical Properties

Cas No. 496807-11-5 SDF
别名 (Rac)-贝拉前列素钠
Canonical SMILES CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@@]2([H])C3=CC=CC(CCCC(O[Na])=O)=C3O[C@@]2([H])C[C@H]1O.[Relative stereochemistry]
分子式 C24H29NaO5 分子量 420.47
溶解度 DMSO: 250 mg/mL (594.57 mM) 储存条件 Store at -20°C
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1 mM 2.3783 mL 11.8915 mL 23.7829 mL
5 mM 0.4757 mL 2.3783 mL 4.7566 mL
10 mM 0.2378 mL 1.1891 mL 2.3783 mL
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Research Update

Beraprost sodium for Pulmonary Hypertension in Dogs: Effect on Hemodynamics and Cardiac Function

Animals (Basel) 2022 Aug 15;12(16):2078.PMID:36009668DOI:10.3390/ani12162078.

Pulmonary hypertension (PH) is a fatal condition that affects many dogs. In humans, PH is often treated with Beraprost sodium (BPS). However, the effectiveness of BPS for canine PH has not been established. This study aimed to evaluate the clinical and cardiovascular response of BPS in canine patients with PH of various causes. Sixteen dogs with PH (post-capillary PH, n = 8; pre-capillary PH, n = 8) were included. BPS was continuously administered twice daily at 15 µg/kg. All dogs underwent echocardiography, including speckle-tracking analysis and blood pressure measurement, before and after BPS administration. Continuous BPS administration (range: 13.2-22.0 µg/kg) significantly decreased the pulmonary and systemic vascular impedance and increased left and right ventricular myocardial strain. In dogs with post-capillary PH, BPS administration caused no significant worsening of the left atrial pressure indicators. No side effects of BPS were observed in any dog. BPS also improved cardiac function and pulmonary circulation through pulmonary vasodilation, suggesting that BPS may be an additional treatment option for canine PH of various causes. Particularly, BPS increased left ventricular function and systemic circulation without worsening the left heart loading condition in dogs with post-capillary PH.

The effects of Beraprost sodium on renal function and cardiometabolic profile in patients with diabetes mellitus: a systematic review and meta-analysis of clinical trials

Int Urol Nephrol 2022 Jan;54(1):111-120.PMID:34019221DOI:10.1007/s11255-021-02887-7.

Purpose: This systematic review and meta-analysis aimed to assess renal function and cardiometabolic biomarkers after treatment with Beraprost sodium in patients with diabetes mellitus. Methods: We systemically searched PubMed, Embase, Scopus, Web of Science, and Cochrane Library up to August 2020. Statistical heterogeneities were computed using Cochrane's Q test and I2 test. A fixed- or random-effects model was used to calculate the weighted mean difference (WMD) and corresponding 95% confidence intervals (CI). Results: From 341citations, seven trials were included into our meta-analysis. Our findings demonstrated that Beraprost sodium intake significantly decreased blood urea nitrogen (BUN) (WMD = -5.62, 95% CI [-8.49, -2.74], P < 0.001) and cystatin C (WMD = -0.57, 95% CI [-0.68, -0.46], P < 0.001). Beraprost sodium intake had no significant effect on fasting blood sugar (FBS), hemoglobin A1c (HbA1c), cholesterol (TC), triglycerides (TG), HDL-C, LDL-C, systolic blood pressure (SBP), diastolic blood pressure (DBP), and creatinine (Cr) in patients with diabetes receiving Beraprost sodium in comparison with the controls. Conclusion: Our meta-analysis revealed that Beraprost sodium administration significantly decreased BUN and cystatin C levels in patients with diabetes. However, no significant effect was observed on the cardiometabolic profile.

Novel effects of Beraprost sodium on vasculatures

Int Angiol 2010 Apr;29(2 Suppl):28-32.PMID:20357746doi

Beraprost sodium (BPS) is a stable orally active prostacyclin analogue with vasodilatory and anti-platelet effects, and has been widely used as therapeutics for pulmonary artery hypertension and chronic arterial obstruction. In order to elucidate its effects on endothelium, we first examined the short-term effects of BPS on nitric oxide (NO) production and endothelial NO synthase (eNOS) activation using bovine aortic endothelial cells. Short-term treatment of BPS induced NO production as well as eNOS phosphorylation at Ser-1179 mediated via cAMP/protein kinase A (PKA) pathway. The effects of BPS on capillary-like tube formation were next determined using human umbilical vein ECs (HUVECs)/normal human dermal fibroblasts co-culture system. BPS was observed to induce capillary-like tube formation mediated via cAMP/PKA pathway, but not via NO generation. Finally, we performed DNA microarray analyses using RNA extracted from BPS treated HUVECs. Interestingly, BPS up-regulated several genes involved in angiogenesis, anti-atherosclerosis, and endothelial function, while down-regulated several genes involved in atherosclerosis. Our data therefore indicate that BPS may be useful not only for patients with pulmonary artery hypertension and chronic arterial obstruction, but also for general atherosclerotic patients complicated with endothelial dysfunction. Further studies are needed to clarify molecular mechanisms of these BPS effects including the involvement of peroxisome proliferator-activated receptor-delta.

[Pharmacological and clinical properties of Beraprost sodium, orally active prostacyclin analogue]

Nihon Yakurigaku Zasshi 2001 Feb;117(2):123-30.PMID:11233303DOI:10.1254/fpj.117.123.

Prostacyclin is an endogeneous eicosanoid synthesized by vascular endothelial cells, and has potent inhibitory effects on platelet adhesion/aggregation and vasoconstriction. However, its therapeutic use is restricted by its extremely short half-life. Beraprost sodium (beraprost) is the first orally active prostacyclin analogue developed by TORAY Industries, Inc. Beraprost possesses a phenol moiety instead of the exo-enol ether moiety, which is the cause of the instability of prostacyclin, and has a modified omega-side chain that contributes to dissociating antiplatelet action from adverse reactions. In 1992, beraprost was approved as a drug for chronic arterial occlusion. Beraprost is now widely used clinically as "Dorner" or "Procylin". The indication for "primary pulmonary hypertension" was also approved in 1999. Recently in Europe, a placebo controlled trial named "Beraprost et Claudication Intermittent-2 (BERCI-2)" was performed, and it was reported that beraprost improved the walking distances of the patients. Beraprost has a variety of biological activities such as antiplatelet effects, vasodilation effects, antiproliferative effects on vascular smooth muscle cells, cytoprotective effects on endothelial cells and inhibitory effects on the production of inflammatory cytokines. On the basis of basic and clinical research, it has been suggested that beraprost is also effective for many intractable diseases. We expect that the relationship between reduced prostacyclin level and these diseases would be clarified and the beneficial effects of beraprost would be demonstrated by controlled clinical trials in the future.

Investigation of Beraprost sodium on Cardiac Function and Hemodynamics in Canine Models of Chronic Pulmonary Hypertension

Front Vet Sci 2022 Apr 14;9:876178.PMID:35498754DOI:10.3389/fvets.2022.876178.

Pulmonary hypertension (PH) is a life-threatening disease in dogs characterized by increased pulmonary arterial pressure (PAP) and/or pulmonary vascular resistance. No study has evaluated the utility of Beraprost sodium (BPS) in dogs with PH. This study aimed to evaluate the effect of BPS on cardiac function and hemodynamics and examine the optimal dose of BPS in canine models of chronic embolic PH. In this prospective crossover study, three doses of BPS (5, 15, and 25 μg/kg, twice a day) were examined in eight canine models of chronic embolic PH. All model dogs underwent invasive PAP measurement, echocardiography, and non-invasive systemic blood pressure measurement before and after continuous administration of oral BPS for 1 week. No side effects of BPS were observed in any dog during the study. All doses of BPS significantly decreased systolic PAP and pulmonary vascular impedance. Additionally, systemic vascular impedance significantly decreased with 15 and 25 μg/kg of BPS. The right ventricular stroke volume and longitudinal strain significantly decreased with all doses of BPS. The left ventricular stroke volume and circumferential strain decreased with 15 μg/kg BPS. BPS was well-tolerated in this study. A dose-dependent vasodilating effect on pulmonary vessels was observed in canine models of chronic PH. Additionally, 15 μg/kg BPS showed a balanced vasodilating effect on systemic and pulmonary vessels. Furthermore, with a decrease in systemic and pulmonary vascular impedance, the left and right ventricular functions were significantly improved. Our results suggest that BPS may be useful in the treatment of canine PH.