2. GPCR/G Protein
  3. Platelet-activating Factor Receptor (PAFR)
  4. Setipafant

Setipafant  (Synonyms: 司替帕泛; BN-50727)

目录号: HY-101675
产品使用指南

摩尔计算器

Setipafant 是一种血小板活化因子 (PAF) 拮抗剂。

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Setipafant Chemical Structure

Setipafant Chemical Structure

CAS No. : 132418-35-0

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Setipafant 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Setipafant is a platelet-activating factor (PAF) antagonist.

IC50 & Target

PAF[1]
体内研究
(In Vivo)

Animals are separated into six groups: U4, controls; S, sham operated animals undergoing laparotomy; I4 and I9, ligation of the mesenteric vessels in the last ileal loop; IT4 and IT9, same procedure together with treatment with Setipafant (50 mg/kg) orally before and after surgery and intraperitoneally during surgery. Animals are killed at day 4 in groups U4, S, I4 and IT4 and at day 9 in groups I9 and IT9, with histological studies and mediator measurements taken. Macroscopic and histological lesions of intestinal wall in groups I4, I9, IT4 and IT9 are similar to those of human neonatal necrotizing enterocolitis and do not vary according to the absence or the presence of Setipafant (BN 50727) treatment. Peritoneal bands are significantly reduced in treated groups IT4 and IT9 as compared with untreated ones I4 and I9. Mucosal PAF levels in the terminal ileum are higher in group I4 than in groups U4 or I9. In the upper loop, mucosal PAF levels are comparable in all groups. An increase in stool PAF levels is observed only in group I9, whereas values comparable to those observed in controls are detected in other groups[1]. Pretreatment of the animals with one or other of the structurally unrelated PAF receptor antagonists, BN 52021 (10 mg/kg, i.p.) or BN 50727 (1 mg/kg, i.p.) significantly reduces Dexamethasone-induced gastric damage. In these animals neither petechiae nor erosions are observed[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

519.02

Formula

C26H23ClN6O2S
CAS 号
中文名称

司替帕泛
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Animal Administration
[1][2]

Piglets[1]
Male and female newborn piglets weighing 1550±31 g are used in all experiments. Six groups are studied. Group U4 is the nonsurgical control group (n=15). No anesthesia is given. Animals are entrusted to their mother and killed at D4. Group S is the sham control group (n=15). At D2 animals undergo laparotomy, intestinal exteriorization, and manipulation for 10 minutes before reintroduction to the abdominal cavity. They are killed at D4. Group I4 consist of animals (n=15) in which ischemia surgery is performed at D2, and animals are killed at D4. Group IT4 consist of animals (n=15) treated as in I4 together with treatment with Setipafant (BN 50727), a PAF receptor antagonist, orally (50 mg/kg of body weight) the day before and daily after surgery until death, and intraperitoneally (50 mg/kg) during surgery. Group I9 consisted of animals (n=15) in which ischemia surgery is performed at D2, and animals are killed at D9. Group IT9 consist of animals (n=15) undergoing the same procedure as in Is together with treatment with Setipafant as in IT4. Another group, U9, is made up of control animals (n=15) that are used only for weight and blood sample studies at D9.
Rats[2]
Male, Wistar rats weighing 160-205 g are used. Between 09 h 00 min and 10 h 00 min each day the animals are given an intraperitoneal injection of the PAF receptor antagonists, BN 52021 (10 mg/kg) or BN 50727(1 mg/kg), or their vehicle, and 30 min later they receive a subcutaneous injection of Dexamethasone sodium phosphate or vehicle. The effectiveness of BN 52021 and BN 50727 treatments is tested in preliminary experiments in anaesthetized (Inactin, 100 mg/kg, i.p.) male rats by injecting 25 and 50 ng/kg PAF into the right femoral vein 30 min before and 30 min after administration of either BN 52021, 10 mg/kg, i.p., or BN 50727, 1 mg/kg, i.p. Mean arterial blood pressure is monitored through a catheter inserted into the right femoral artery by an electromanometer using a Statham P23 dB pressure transducer.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Setipafant 相关分类

  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Setipafant132418-35-0BN-50727司替帕泛BN50727BN 50727Platelet-activating Factor Receptor (PAFR)Inhibitorinhibitorinhibit

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