CV-6209 (chloride)
目录号 : GC43333A potent PAF receptor antagonist
Cas No.:100488-87-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor, inhibiting aggregation of rabbit and human platelets induced by PAF with IC50 values of 75 and 170 nM, respectively. It has little action on platelet aggregation induced by arachidonic acid, ADP, or collagen. CV-6209 is bioavailable, as it prevents PAF-induced hypotension in rats, while not blocking hypotension triggered by arachidonic acid , histamine, bradykinin , or isoproterenol . CV-6209 is used to study the role of PAF receptor signaling in vitro and in vivo.
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5569 mL | 7.7845 mL | 15.569 mL |
| 5 mM | 0.3114 mL | 1.5569 mL | 3.1138 mL |
| 10 mM | 0.1557 mL | 0.7785 mL | 1.5569 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
CV-6209, a highly potent antagonist of platelet activating factor in vitro and in vivo
J Pharmacol Exp Ther 1987 Jul;242(1):263-8.PMID:3612533doi
2-[N-acetyl-N-(2-methoxy-3-octadecylcarbamoyloxypropoxycarbonyl) aminomethyl]-1-ethylpyridinium chloride (CV-6209) inhibited aggregation of rabbit and human platelets induced by platelet activating factor (PAF) with the IC50 values of 7.5 X 10(-8) and 1.7 X 10(-7) M, respectively, and had little effects on the aggregation induced by arachidonic acid, ADP and collagen. The inhibitory effect of CV-6209 on the PAF-induced rabbit platelet aggregation was 104, 9, 8 and 3 times more potent than the PAF antagonists CV-3988, ONO-6240, Ginkgolide B and etizolam, respectively. CV-6209 inhibited [3H]serotonin release from rabbit platelets stimulated with PAF (3 X 10(-8) M) with a similar potency as the inhibition on the platelet aggregation. CV-6209 inhibited PAF (0.3 microgram/kg i.v.)-induced hypotension in rats (ED50, 0.009 mg/kg i.v.) with no effect on the hypotension induced by arachidonic acid, histamine, bradykinin and isoproterenol. CV-6209 (1 mg/kg) inhibited slightly the acetylcholine-induced hypotension. In rats, post-treatment with CV-6209 reversed the PAF (1 microgram/kg i.v.)-induced hypotension rapidly (ED50, 0.0046 mg/kg i.v.); CV-6209 was 74, 20, 185 and over 2100 times more potent than CV-3988, ONO-6240, Ginkgolide B and etizolam, respectively. Thus, the relative potency of the anti-PAF action of PAF analog (CV-6209, CV-3988 and ONO-6240) differed little between the inhibition of PAF-induced platelet aggregation and the reversal of PAF-induced hypotension, but that of nonPAF analogs (Ginkgolide B and etizolam) differed greatly with these assay systems, when standardized with CV-6209.(ABSTRACT TRUNCATED AT 250 WORDS)
Effects of the platelet-activating factor antagonists CV-6209 and CV-3988 on nephrotoxic serum nephritis in the rat
Nephron 1992;60(4):471-6.PMID:1584324DOI:10.1159/000186811.
Platelet-activating factor (PAF) is known as an important mediator in the pathogenesis of glomerular injury. In the present study, we evaluated the effect of the specific PAF antagonists CV-6209 and CV-3988 on accelerated nephrotoxic serum nephritis (NTN) in the rat. The amount of urinary protein excretion was significantly less in the rats treated with CV-6209 or CV-3988 on the 5th and 7th day of treatment than in the nontreated controls. The results of light- and immunofluorescence-microscopic examination did not demonstrate any favorable effect on glomerular changes by these PAF antagonists. However, CV-6209 protected against the loss of glomerular anionic charges in rats with NTN. Thus, it is suggested that PAF is a potent mediator of protein excretion, and that the loss of glomerular anionic charges is an important mechanism for the mediation of PAF in glomerulonephritis.
Effects of the PAF-analog and -antagonist CV-6209 on cultured human glioma cell lines
Prostaglandins Leukot Essent Fatty Acids 1991 Jun;43(2):103-10.PMID:1886907DOI:10.1016/0952-3278(91)90180-d.
Cell lines of human glioma (U-343 MGa and U-251 MG) and human glia (U-533 CG) origin were cultured as monolayers and exposed to CV-6209, an alkyl-phospholipid analog and antagonist of platelet activating factor. This drug had very potent antiproliferative effects on the studied human glioma cell lines; IC50 was 0.9 microM after 48 h treatment and 0.2 microM after 2 weeks treatment. At these doses no growth inhibitory effect was noted on the normal glia cells. The effects on the glioma cells were reversible in the dose intervals, where cell proliferation, 3H-thymidine and 14C-methionine uptakes were greatly inhibited. The simultaneous administration of platelet activating factor [(R)PAF] did not influence the antiproliferative effects of CV-6209 on the cells cultured as monolayers. The structurally similar analog CV-3988 also had antiproliferative effects, although at 10 times higher concentration than CV-6209. Two other, structurally unrelated, PAF-antagonists (WEB-2086 and TCV-309) gave effects only at very high concentrations. The U-343 MGa cell line was also exposed to CV-6209 when growing as multicellular spheroids. The studies on the spheroid cultures also demonstrated good antitumoral effects with decreases of both the volume growth and the thymidine uptake. The simultaneous administration of (R)PAF reversed the inhibitory effect of CV-6209 on thymidine incorporation. This study demonstrates a strong antitumoral effect at low concentrations of CV-6209. The antiproliferative effects were probably primarily related to the ether-lipid structure and not to the PAF-antagonistic properties. The good antitumoral effect of CV-6209 on both monolayer and spheroid cultures and the possible PAF-antagonistic properties are discussed.
The effect of CV-3988 and CV-6209 on the acute gastric erosions of rats due to water-immersion and restraint stress
Lipids 1991 Dec;26(12):1354-5.PMID:1819732DOI:10.1007/BF02536565.
CV-3988 and CV-6209 inhibited gastric erosions in rats due to water-immersion and restraint stress in a dose-dependent manner. The above inhibitory effects of CV-3988 were observed in the presence of indomethacin, which may indicate that the inhibition is not prostaglandin dependent. The studies indicate that platelet-activating factor may be involved in the formation of erosions in rats under water-immersion and restraint stress.
Comparative study of the effect of CV-6209, a specific PAF-antagonist, on rat paw edema caused by different phlogogen agents
Pharmacology 1990;40(4):211-7.PMID:1697076DOI:10.1159/000138661.
Comparative effects of CV-6209, a potent and specific platelet activating factor (PAF) antagonist, on PAF-acether-, carrageenin-, histamine-, serotonin-, compound 48/80-, dextran-, zymosan A- and arachidonic acid-induced rat paw edema were investigated. CV-6209 has proven to be effective in PAF-induced edema, but it also showed a significant activity in other models of paw edema, except those induced by zymosan A and arachidonic acid. Other drugs tested, namely indometacin, mepyramine, methysergide and nordihydroguaiaretic acid showed a more selective inhibitory profile. These results suggest an important role of PAF in the inflammatory process caused by intraplantar injection of different phlogogenes in the rat paw.