Ginkgolide B

製品コードS1343 バッチS134308

印刷

化学情報

 Chemical Structure Synonyms BN52021 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C20H24O10

分子量 424.4 CAS No. 15291-77-7
Solubility (25°C)* 体外 DMSO 85 mg/mL (200.28 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

2.500mg/ml (5.89mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Ginkgolide B (BN52021) is a PAFR antagonist with IC50 of 3.6 μM.
in vitro Ginkgolide B potently inhibits a platelet-activating factor (PAF) receptor. [1] Treatment of PMN with this compound (0.5 μM -12 μM) stimulates a rapid and weak production of reactive oxygen species determined by chemiluminescence. It potentiates the CL response induced by fMet-Leu-Phe and zymosan. [2] This chemical induces cyst cell differentiation and alteres the Ras/MAPK signaling pathway. [3] It promotes the proliferation and endothelial gene expression, and markedly enhances vascular endothelial growth factor-induced migration response and the capability to incorporate into the vascular networks in EPCs. It protects EPCs from H2O2-induced cell death. It induces the phosphorylation of eNOS, Akt and p38, which in turn promotes cell proliferation and function. [4]
in vivo Ginkgolide B (2 μM) significantly inhibits MDCK cyst formation dose dependently, with up to 69% reduction. This compound also significantly inhibits cyst enlargement in the MDCK cyst model, embryonic kidney cyst model, and PKD mouse model.[3] Preischemic application of this compound (50 mg/kg p.o.) significantly reduces neuronal damage.[5] 30 minutes of pretreatment with this chemical (100 mg/kg, s. c.) reduces the infarct area in the mouse model of focal ischemia. In primary cultures of hippocampal neurons and astrocytes from neonatal rats, this compound (1 μM) protects the neurons against damage caused by glutamate. It (100 μM) reduces apoptotic damage induced by staurosporine. [6] In pentobarbitone or ethyl carbamate-anaesthetized animals, this compound (1 mg/kg i.v. or 10 mg/kg p.o.) inhibits bronchoconstriction, the hematocrit increase and the accompanying thrombopenia and leukopenia induced by PAF-acether (33 ng/kg–100 ng/kg). It at a dose of 3 mg/kg reduces the bronchoconstriction induced by aerosolized PAF-acether. This compound at a dose of 300 μM also inhibits the superoxide production by PAF-acether-stimulated alveolar macrophages. It blocks the formation of thromboxane-triggered by PAF-acether (100 ng) injected into perfused lung.Pretreatment of parenchyma lung strips with this chemical (100 μM) partially inhibits the contraction induced by PAF-acether (0.1 μM) and suppresses the accompanying release of thromboxane. [7] This compound inhibits the maturation of ischemic injury. [8] It treatment reveals marked reduction in infarction volume, brain edema and neurological deficits. This compound also inhibitsischemia/reperfusion (I/R) induced NF-κB, microglia activation and production of pro-inflammatory cytokines. It reducesBax protein levels and increases Bcl-2 protein levels in the post-ischemic brains. [9] This chemical attenuates platelet aggregation and inhibits phosphatidylinositol 3 kinase (PI3K) activation and Akt phosphorylation in thrombin- and collagen-activated platelets.It decreases plasma PF4 and RANTES levels in ApoE−/− mice.This compound diminishes P-selectin, PF4, RANTES, and CD40L expression in aortic plaque in ApoE−/− mice.Moreover, it suppresses macrophage and vascular cell adhesion protein 1 (VCAM-1) expression in aorta lesions in ApoE−/− mice.[10]

プロトコル(参考用のみ)

動物実験 動物モデル Eight-week-old male ApoE−/− mice
投薬量 0.6 mg/day
投与方法 Intragastric administration

参考

  • https://pubmed.ncbi.nlm.nih.gov/2820421/
  • https://pubmed.ncbi.nlm.nih.gov/22338085/
  • https://pubmed.ncbi.nlm.nih.gov/21623570/
  • https://pubmed.ncbi.nlm.nih.gov/2298830/
  • https://pubmed.ncbi.nlm.nih.gov/13130383/
  • https://pubmed.ncbi.nlm.nih.gov/3019727/
  • https://pubmed.ncbi.nlm.nih.gov/2846788/
  • https://pubmed.ncbi.nlm.nih.gov/22850444/
  • https://pubmed.ncbi.nlm.nih.gov/22662117/

カスタマーフィードバック

, , Mol Neurobiol, 2015, 53(5):3448-3461

Data from [Data independently produced by , , Oncotarget, 2017, 8(8): 13846-13854]

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Exposure-Response Analysis and Mechanism of Ginkgolide B's Neuroprotective Effect in Acute Cerebral Ischemia/Reperfusion Stage in Rat [ Biol Pharm Bull, 2022, 45(4):409-420] PubMed: 35370265
Ginkgolide B Regulates CDDP Chemoresistance in Oral Cancer via the Platelet-Activating Factor Receptor Pathway [ Cancers (Basel), 2021, 13(24)6299] PubMed: 34944919
Bovine Respiratory Syncytial Virus Enhances the Adherence of Pasteurella multocida to Bovine Lower Respiratory Tract Epithelial Cells by Upregulating the Platelet-Activating Factor Receptor [ Front Microbiol, 2020, 11:1676] PubMed: 32849350
Bovine Respiratory Syncytial Virus Enhances the Adherence of Pasteurella multocida to Bovine Lower Respiratory Tract Epithelial Cells by Upregulating the Platelet-Activating Factor Receptor [ Front Microbiol, 2020, 11:1676] PubMed: 32849350
PAFR selectively mediates radioresistance and irradiation-induced autophagy suppression in prostate cancer cells. [Yao B, et al. Oncotarget, 2017, 8(8):13846-13854] PubMed: 28099922
Attenuated Reactive Gliosis and Enhanced Functional Recovery Following Spinal Cord Injury in Null Mutant Mice of Platelet-Activating Factor Receptor [Wang Y, et al. Mol Neurobiol, 2015, 10.1007/s12035-015-9263-6] PubMed: 26084439

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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