GLPBio

CV-6209 (chloride)

Catalog No.: GC43333Purity:>98.00%
COASDSData Sheet
CV-6209 (chloride) is a potent antagonist of the platelet-activating factor (PAF) receptor with the IC50 value of 75nM for rabbit platelets.

Products are for research use only. Not for human use. We do not sell to patients.

CV-6209 (chloride)
Cas No.: 100488-87-7
1mgIn Stock
$94.00
1
5mgIn Stock
$249.00
1
10mgIn Stock
$399.00
1
25mgIn Stock
$639.00
1
50mgIn Stock
$875.00
1
100mgIn Stock
$1,170.00
1
500mgIn Stock
$2,630.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citations

No citations are currently available for this product. Below are selected publications citing GlpBio products.
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

Description

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.

Protocol

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:
[1] 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.
[2] 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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
100488-87-7
SMILES
O=C(C)N(C(OCC(OC)COC(NCCCCCCCCCCCCCCCCCC)=O)=O)CC1=CC=CC=[N+]1CC.[Cl-]
Molecular Formula
C34H60N3O6•Cl
Molecular Weight
642.3
Solubility
Water: 10 mg/ml
Storage
4°C, sealed storage, away from moisture
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

Reviews

Review for CV-6209 (chloride)

Rating: 5
  • 5 Star100%
  • 4 Star0%
  • 3 Star0%
  • 2 Star0%
  • 1 Star0%