There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Type 3 cyclic nucleotide phosphodiesterase (PDE-3) isoforms exhibit a high affinity ("low K(m)") for cAMP and are specifically inhibited by cGMP and a number of pharmacological agents. The PDE-3 family consists of at least two isozymes, PDE-3A (cardiac type) and PDE-3B (adipocyte type), with distinct tissue-specific distributions[3]. Cilostazol is a 2-oxo-quinoline derivative with antithrombotic, vasodilator, antimitogenic and cardiotonic properties. The compound is a potent inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system (IC50: 0.2 μM). There is no relevant effect by cilostazol on PDE 1, 2 and 4 at comparable concentrations, and only a minor effect on PDE 5 (IC50: 5 ± 8 mM). In addition, there was inhibition of adenosine uptake, eventually resulting in changes in cAMP levels[4]. In vitro, cilostazol inhibited adenosine uptake into cardiac myocytes, coronary artery smooth muscle cells and endothelial cells, with a median effective concentration of 10 μM, which might result from stimulation of adenosine A1 receptors and might counteract the increase of cAMP via PDE-inhibition[4]. Cilostazol inhibits platelet aggregation and has considerable antithrombotic effects in vivo. The compound relaxed vascular smooth muscle and inhibited mitogenesis and migration of vascular smooth muscle cells and decreaseed levels of serum triglycerides and caused some increase in HDL-cholesterol levels[4]. In the rat carotid injury model, single local application of cilostazol resulted in a marked inhibition of intima proliferation. Interestingly, the tissue concentration of cilostazol in the carotid artery and muscle around the carotid artery was considerably higher than in plasma, which was probably related to its highly lipophilic nature. There was also suppression of neointimal formation in dog grafted veins, which appeared to be related to inhibition of angiotensin II forming enzymes[4].
Cilostazol/西洛他唑 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rat articular chondrocytes
30 μM
24 h
Cilostazol pre-treatment protected articular chondrocytes from oleate-induced lipoapoptosis by upregulating PKCK2 expression and reversed the oleate-induced decrease in FSP27 protein expression level.
Bone Res. 2018 Jul 6;6:20.
Rat primary vascular smooth muscle cells
10 μM
60 min
To investigate the effect of Cilostazol on BAY-induced VASP phosphorylation. Results showed that Cilostazol significantly reduced BAY-mediated VASP Ser239 phosphorylation.
Front Pharmacol. 2012 Feb 7;3:10.
Human peripheral blood mononuclear cell (PBMC) basophils
100 µM
30 min
To study the effect of PDE3 inhibitors on basophil degranulation, results showed that Cilostazol was able to impair basophil degranulation.
Front Pharmacol. 2020 May 1;11:470.
A7r5 rat vascular smooth muscle cells
100 and 200 μM
24 h
To investigate the effect of cilostazol on HG-induced dysfunction in A7r5 cells, the results showed that cilostazol significantly suppressed the expressions of RAGE, FAK, MMP-2, ICAM-1, and VCAM-1, and reversed cell proliferation, adhesion, and migration.
J Biomed Sci. 2019 Sep 6;26(1):68.
Cilostazol/西洛他唑 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Tauopathy model
Intraperitoneal injection
3 mg/kg
Twice daily for 30 days
Cilostazol enhanced proteasome function via the cAMP/PKA pathway, reduced tau accumulation, and attenuated tauopathy and cognitive decline.
Transl Res. 2018 Mar;193:31-41
Mice
Tg2576 transgenic mice
Oral
0.01%
Daily, for 7-9 months
To investigate whether lower-dose cilostazol can decrease micro-hemorrhages and Aβ deposition in the brain of Tg2576 mice. Results showed that the CAA score was significantly lower in the cilostazol group compared to the control group at 21-23 months, indicating that lower-dose cilostazol can reduce the vascular amyloid burden.
Int J Mol Sci. 2020 Mar 26;21(7):2295
CD-1 mice
Stable closed femoral fracture model
Oral gavage
30 mg/kg
Daily administration for 2 or 5 weeks
Cilostazol accelerates fracture healing and induces bone formation in aged mice by stimulating angiogenesis and increasing the expression of PI3K and RUNX2.
Int J Mol Sci. 2024 Jan 6;25(2):755
Mice
High-fat diet-induced osteoarthritis model
Oral
30 mg·kg-1
Once daily for 10 weeks
Cilostazol significantly reduced high-fat diet-induced cartilage degeneration and increased the population of PKCK2-, STAMP2-, and FSP27-positive chondrocytes.
Bone Res. 2018 Jul 6;6:20.
Mice
ApoE null mice
Dietary supplementation
0.1%
16 weeks
Co-treatment of cilostazol with GbE significantly reduced atherosclerotic lesion area in ApoE null mice and decreased the expression of inflammatory cytokines and adhesion molecules.
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