CV-6209 (chloride)是一种强效的血小板活化因子受体拮抗剂，对兔血小板的IC50值为75nM。
Cas No.:100488-87-7
Sample solution is provided at 25 µL, 10mM.
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CV-6209 (chloride) is a potent antagonist of the platelet-activating factor (PAF) receptor with the IC50 value of 75nM for rabbit platelets [1]. CV-6209 can attenuate the gastric mucosal injury induced by ischemia-reperfusion, and inhibit both an increase of thiobarbituric acid reactive substances and a decrease of α-tocopherol in gastric mucosa after ischemia-reperfusion [2]. CV-6209 has been widely used to inhibit the growth of Helicobacter pylori, as well as to suppress the bacterial motility and adhesion[3].
In vitro, CV-6209 treatment for 48h significantly inhibited the proliferation of U-343 MGa cells, with an IC50 value of 0.9μM[4]. Treatment of rat peritoneal macrophages with 10µM CV-6209 for 8 hours significantly inhibited the production of TNF-α induced by thapsigargin (46.1nM)[5].
In vivo, CV-6209 treatment via intraperitoneal injection at a dose of 0.2mg (dissolved in 0.2ml of physiological saline) every 8 hours for 6 days prevented pre-implantation thrombocytopenia in pregnant mice and reduced the number of implantation sites. [6]. One hour before aortic occlusion, a single intravenous dose of 1mg/kg of CV-6209 was administered, which effectively prevented cardiopulmonary ischemia-reperfusion injury in pigs[7]. A single intravenous injection of 1mg/kg dose of CV-6209 lasted for 1 minute, significantly alleviating the increase in portal venous pressure (PVP) caused by endotoxin in rats, and completely inhibiting hypotension[8].
References:
[1] Terashita Z I, Imura Y, Takatani M, et al. CV-6209, a highly potent antagonist of platelet activating factor in vitro and in vivo[J]. The Journal of pharmacology and experimental therapeutics, 1987, 242(1): 263-268.
[2] Yoshikawa T, Takahashi S, Naito Y, et al. Effects of a platelet-activating factor antagonist, CV-6209, on gastric mucosal lesions induced by ischemia-reperfusion[J]. Lipids, 1992, 27(12): 1058-1060.
[3] Iwao Y, Takano T, Taneike I, et al. Anti-Helicobacter pylori actions of CV-6209, a platelet-activating factor receptor antagonist[J]. The Journal of General and Applied Microbiology, 2013, 59(2): 147-152.
[4] Gati I, Bergström M, Muhr C, et al. Effects of the PAF-analog and-antagonist CV-6209 on cultured human glioma cell lines[J]. Prostaglandins, leukotrienes and essential fatty acids, 1991, 43(2): 103-110.
[5] Yamada M, Ichinowatari G, Tanimoto A, et al. Inhibition of tumor necrosis factor-α production by SK&F 98625, a CoA-independent transacylase inhibitor, in cultured rat peritoneal macrophages[J]. Life sciences, 1998, 62(20): PL297-PL302.
[6] Ando M, Suginami H, Matsuura S. Pregnancy Suppression by a Structurally Related Antagonist for Platelet Activating Factor, CV‐6209, in Mice[J]. Asia‐Oceania Journal of Obstetrics and Gynaecology, 1990, 16(3): 283-290.
[7] Qayumi K A, English J C, Feeley E J E, et al. A new platelet-activating factor antagonist (CV-6209) in preservation of heart and lung for transplantation[J]. Cardiovascular drugs and therapy, 1997, 11(6): 777-785.
[8] Kitagawa S, Kubota Y, Yamaguchi T, et al. Role of endogenous platelet‐activating factor (PAF) in endotoxin‐induced portal hypertension in rats[J]. Journal of gastroenterology and hepatology, 1992, 7(5): 481-485.
CV-6209 (chloride)是一种强效的血小板活化因子受体拮抗剂，对兔血小板的IC50值为75nM[1]。CV-6209可减轻缺血再灌注诱导的胃黏膜损伤，并抑制缺血再灌注后胃黏膜中thiobarbituric acid反应物质的增加和α-tocopherol的减少[2]。CV-6209已被广泛用于抑制幽门螺杆菌的生长以及抑制细菌的运动和粘附[3]。
在体外，CV-6209处理48小时显著抑制了U-343 MGa细胞的增殖，IC50值为0.9μM[4]。用10μM的CV-6209处理大鼠腹腔巨噬细胞8小时，显著抑制了thapsigargin (46.1nM)诱导的TNF-α的产生[6]。
在体内，每8小时腹腔注射0.2mg的CV-6209（溶于0.2ml生理盐水），连续6天，可预防孕鼠着床前血小板减少症并减少着床点数[6]。在主动脉阻断前1小时，单次静脉注射1mg/kg剂量的CV-6209，有效预防了猪的心肺缺血再灌注损伤[7]。单次静脉注射1mg/kg剂量的CV-6209持续1分钟，显著减轻了内毒素引起的大鼠门静脉压力升高，并完全抑制了低血压[8]。
| Cell experiment [1]: | |
Cell lines | Rat peritoneal macrophages |
Preparation Method | The rat peritoneal macrophages were suspended in Eagle’s minimal essential medium containing 10% calf serum, penicillin G potassium (18µg/ml), and streptomycin sulfate (50µg/ml). The macrophages were seeded at a density of 6×106 cells per 60mm plastic tissue culture dish in 4ml of medium and incubated for 2h at 37°C. The dishes were then washed three times to remove nonadherent cells. The adherent cells were incubated for 20h at 37°C in 4ml of medium, washed three times with medium containing no serum. The cells were incubated for 8h at 37°C in 4 ml of medium containing different concentrations of CV-6209 (0, 0.1, 1, and 10µM) in the presence of thapsigargin (46.1nM). The concentration of TNF-α in cells was measured. |
Reaction Conditions | 0, 0.1, 1, and 10µM; 8h |
Applications | CV-6209 treatment significantly reduced the TNF-α levels in rat peritoneal macrophages induced by thapsigargin in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Wistar rat |
Preparation Method | Male Wistar rats, weighing 280-300g, were fasted for 24h before experiments but allowed free access to water. The rats were anaesthetized with urethane (1.2g/kg; s.c.) and were placed supinely on an operating table. A tracheotomy was performed, and a polyethylene tube was inserted to ensure a free airway. Rectal temperature was maintained at 37°C using a heating pad during the experiment. The right carotid artery was cannulated with a 24-gauge plastic catheter. The catheter was connected to a pre-calibrated pressure transducer via a saline-filled tube, and the blood pressure (BP) was recorded. The abdomen was mid-incised, and the portal vein was catheterized via the ileocolic vein using a 27-gauge catheter. After verifying that free reflux of blood was obtained, the catheter was interposed by a three-way connector and then connected to a saline-filled tube. Saline (0.6mL/100g/h) was infused continuously through the tube using an infusion pump, and the PVP was measured simultaneously using a pre-calibrated pressure transducer. The zero-reference point was established 1cm above the operating table. The three-way connector was used for intravenous administrations of PAF, endotoxin, CV-6209 or vehicle solution of each experiment for 1min using a capillary infusion pump, and therefore, PVP monitoring was discontinued during the intravenous administrations. CV-6209 was dispersed in physiologic saline. Six rats received pretreatment with CV-6209 (1mg/kg) 20min before intravenous administration of endotoxin (2mg/kg, 0.1ml in physiologic saline). Six rats (controls) received intraportal administration of the vehicle (saline) 20min after pretreatment with CV-6209. BP and PVP were monitored continuously for a further 60min after each treatment. |
Dosage form | 1mg/kg for once; i.v. |
Applications | CV-6209 treatment significantly alleviated the endotoxin-induced elevation of PVP and completely inhibited the low BP in rats. |
References: | |
| Cas No. | 100488-87-7 | SDF | |
| Canonical SMILES | O=C(C)N(C(OCC(OC)COC(NCCCCCCCCCCCCCCCCCC)=O)=O)CC1=CC=CC=[N+]1CC.[Cl-] | ||
| 分子式 | C34H60N3O6•Cl | 分子量 | 642.3 |
| 溶解度 | Water: 10 mg/ml | 储存条件 | 4°C, sealed storage, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5569 mL | 7.7845 mL | 15.569 mL |
| 5 mM | 311.4 μL | 1.5569 mL | 3.1138 mL |
| 10 mM | 155.7 μL | 778.5 μL | 1.5569 mL |
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