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普侖司特

普侖司特

中文名稱普侖司特
中文同義詞半水普侖司特;普侖司特水合物;普魯司特半水合物;普魯司特 水合物;化合物 PRANLUKAST HEMIHYDRATE;普倫司特半水合物
英文名稱8-[4(4-phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran
英文同義詞PRANLUKASTHEMIHYDRATE;8-[4(4-phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran;N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-benzamide hemihydrate;Pranlukast hemihydrate >=98% (HPLC), white solid;Benzamide,N-[4-oxo-2-(2H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-,hydrate (2:1);N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phe...;Pranlukast hydrateQ: What is Pranlukast hydrate Q: What is the CAS Number of Pranlukast hydrate Q: What is the storage condition of Pranlukast hydrate;N-[4-oxo-2-(2H-tetrazol-5-yl)chromen-8-yl]-4-(4-phenylbutoxy)benzamide,hydrate
CAS號150821-03-7
分子式C27H25N5O5
分子量499.53
EINECS號
相關(guān)類別合成
Mol文件150821-03-7.mol
結(jié)構(gòu)式普侖司特 結(jié)構(gòu)式

普侖司特 性質(zhì)

儲存條件-20°C
溶解度二甲基亞砜:≥10mg/mL
形態(tài)白色固體
顏色白色至米白色

普侖司特 用途與合成方法

Pranlukast hemihydrate (ONO-1078 hemihydrate) 是一種高效的競爭性的選擇性 leukotriene 拮抗劑。Pranlukast 抑制 [3H]LTE4,[3H]LTD4 和 [3H]LTC4 與肺膜結(jié)合,Ki 分別為 0.63±0.11,0.99±0.19 和 5640±680 nM。

LTE 4

0.63 nM (Ki)

LTD 4

0.99 nM (Ki)

LTC 4

5640 nM (Ki)

In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [ 3 H]LTE 4 , [ 3 H]LTD 4 , and [ 3 H]LTC 4 bindings to lung membranes with K i s of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [ 3 H]LTD 4 binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC 4 - and LTD 4 -induced contractions of guinea pig trachea and lung parenchymal strips with a pA 2 range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC 4 to LTD 4 , Pranlukast also antagonizes the LTC 4 -induced contraction of guinea pig trachea (pA 2 =7.78). Pranlukast significantly reverses the LTD 4 -induced prolonged contraction without effect on the KCl- and BaCl 2 -induced contractions of guinea pig trachea. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT 1 receptors is inhibited by pretreatment with the CysLT 1 receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT 1 receptor antagonist Pranlukast and the 5-lipoxygenase inhibitor Zileuton on translocation are also assessed. The results show that Pranlukast, but not Zileuton, inhibits the translocation of the CysLT 1 receptor 6 h after OGD.

Carrageenan (CAR, 5 mg per mouse) is injected i.p. 24 h before LPS (50 p,g per mouse) is injected i.v. Various doses of Pranlukast (ONO-1078; 40, 20, and 10 mmol/kg), AA-861 (20, 10, and 5 mmol/kg), Indomethacin (40 mmollkg), and the controls are injected s.c. into mice 30 min before they are challenged with 50 p,g of LPS. The maximum soluble doses are 0.6 mmol/mL in 10% DMSO for AA-861 and 1.2 mmol/mL in 10% ethanol for Pranlukast. These solutions are used as the maximum doses for the treatments. The mortality of mice is significantly decreased in AA-861- Pranlukast-treated mice relative to that in the control mice. Pretreatment with CAR (5 mg i.p.) renders the mice more sensitive to the effect of LPS. Although the survival rate of mice treated with each solvent is 20% at 72 h after LPS (50 p,g per mouse) administration, s.c. treatment with AA-861 (20 mmol/kg) or Pranlukast (40 mmol/kg) significantly increases the survival rate after the LPS administration (AA-861, P<0.001; Pranlukast, P<0.01).

安全信息

危險品標(biāo)志Xn
危險類別碼22-36/37/38
安全說明26-36/37
WGK Germany3
危險等級IRRITANT

MSDS信息

更新日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/08HY-B0290A普侖司特
Pranlukast hemihydrate
150821-03-750mg600元
2025/02/08HY-B0290A普侖司特
Pranlukast hemihydrate
150821-03-710mM * 1mLin DMSO660元

普侖司特 上下游產(chǎn)品信息

"普侖司特"相關(guān)產(chǎn)品信息
普侖司特 氟哌啶醇 扎魯司特 3-氨基-2-羥基苯乙酮
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