2. Immunology/Inflammation
  3. Thrombopoietin Receptor
  4. AH23848

AH23848 (compound 6) 是血栓素 A2 受体竞争性阻滞剂，也具有口服活性，其针对人靶点的 IC50 值范围为50 nM，且作用持续时间长。AH23848 对其他前列腺素、5-羟色胺 (5-HT) 或腺苷二磷酸 (ADP) 受体无活性。AH23848 可用于闭塞性血管疾病的研究。

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AH23848

AH23848 Chemical Structure

CAS No. : 81443-73-4

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AH23848 的其他形式现货产品:

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AH23848 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AH23848 (compound 6) is a competitive blocker of the thromboxane A2 receptor and an orally effective agent, with an IC50 value of 50 nM against human targets and a long duration of action. AH23848 shows no activity against other prostaglandin, serotonin (5-HT) or adenosine diphosphate (ADP) receptors. AH23848 can be used in the research of occlusive vascular diseases[1].

体外研究
(In Vitro)

AH23848 (compound 6) (3.0×10-8-3.0×10-6 mol/liter; 30 min) 在离体人肺动脉平滑肌中作为血栓素 A2 受体的竞争性拮抗剂，其 pA2 为 7.8[1]。
AH23848 (6.0×10-8-6.0×10-6 mol/liter; 1.0×10-5 mol/liter) 可竞争性拮抗离体大鼠主动脉平滑肌中的血栓素 A2 受体，其 pA2 为 7.94；且在最高达 1.0×10-5 mol/liter 的浓度下，不会阻断 5-HT 或氯化钾诱导的收缩[1]。
AH23848 (1.0×10−6 mol/liter) 不会阻断 PGE2 或 PGF2α 诱导的离体非血管平滑肌标本收缩[1]。
AH23848 (1.0×10-7-1.0×10-4 mol/liter) 可强效且特异性地抑制人富血小板血浆中血栓烷受体依赖性的血小板聚集，针对不同激动剂的 IC50 值范围为 1.05×10-7 至 6.3×10-7 mol/liter，且不会阻断由 ADP、5-HT 或肾上腺素诱导的聚集[1]。

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

AH23848 相关抗体:
体内研究
(In Vivo)

AH23848 (静脉推注单次给药，剂量 0.03-1.0 mg/kg) 可强效且特异性地抑制麻醉豚鼠中胶原诱导的血栓栓塞和支气管收缩反应，在静脉给药剂量高达 1.0 mg/kg 时对 ADP 诱导的血小板减少无影响[1]。
AH23848 (0.01-0.3 mg/kg；静脉注射；单次推注) 可特异性拮抗 U-46619 在麻醉 Beagle 犬中诱导的肠系膜血管收缩，且不改变基线血流动力学参数；在 0.1 mg/kg i.v 剂量下，可使 U-46619 的剂量反应曲线右移 6.5 倍[1]。
AH23848 (1 mg/kg；灌胃；单次给药) 可在清醒 Beagle 犬中产生持续、特异性的胶原诱导血小板聚集抑制作用，其峰值效应使胶原剂量反应曲线右移 23 倍，残余活性至少持续 11 小时[1]。

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

Animal Model: Guinea pig (anesthetized)[1]
Dosage: 0.03 mg/kg (collagen-induced responses); 1.0 mg/kg (ADP-induced thrombocytopenia)
Administration: i.v.; single bolus
Result: Substantially reduced collagen-induced thrombocytopenia.
Almost completely abolished the collagen-induced diastolic pressor response.
Nearly eliminated collagen-induced bronchoconstriction.
Showed no inhibitory effect on ADP-induced thrombocytopenia at 1.0 mg/kg.
Animal Model: Beagle dog (anesthetized)[1]
Dosage: 0.01-0.3 mg/kg
Administration: i.v.; single bolus
Result: Had little or no effect on baseline blood pressure or mesenteric arterial blood flow.
Specifically antagonized U-46619-induced mesenteric vasoconstriction.
Produced a mean 6.5-fold rightward shift in the U-46619 dose-effect curve at 0.1 mg/kg.
Animal Model: Beagle dog (conscious)[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose
Result: Produced a marked inhibition of collagen-induced platelet aggregation ex vivo, with a mean peak 23-fold rightward shift of the collagen concentration-aggregation curve.
Showed a residual twofold rightward shift still evident 11 hours after dosing.
Had no inhibitory effect on ADP-induced platelet aggregation ex vivo.
分子量

477.60

Formula

C29H35NO5
CAS 号
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

AH23848 相关分类

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  • 稀释计算器

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Keywords:

AH2384881443-73-4AH 23848AH-23848Thrombopoietin Receptorhuman pulmonary artery smooth muscle5-HT receptorsrat aorta smooth muscleocclusive vascular diseaseguinea pigsthromboxane A2 receptordog saphenous vein smooth muscleprostanoid receptorshuman plateletsADP receptorsInhibitorinhibitorinhibit

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目录号：
HY-10419
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