2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor mAChR
  4. HY-078020

HY-078020 (compound III-4) 是一种具有选择性的，口服有效的 histamine H1 受体拮抗剂 (H1R)， IC50 值为 24.12 nM。HY-078020 在过敏性疾病中具有抗炎作用。

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HY-078020 Chemical Structure

HY-078020 Chemical Structure

CAS No. : 2756222-90-7

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HY-078020 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

HY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases[1].

IC50 & Target

H1 Receptor

24.12 nM (IC50)

mAChR3

 

体外研究
(In Vitro)

HY-078020 对 H1R 具有强效抑制活性 (IC50 是 24.12 nM)，对 M3R 和 hERG 抑制作用较弱，IC50 分别为 >10 和 17.6 μM[1]。
HY-078020 具有适度的渗透性 (流出率 <2)，肝微粒体稳定性，在人、比格犬和小鼠 (T1/2 = 86.625 min) 体内表现出较长的半衰期[1]。
HY-078020 对大鼠 cytochrome P450 (CYP) 同工酶 CYP3A4 具有抑制作用[1]。

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

HY-078020 相关抗体:
体内研究
(In Vivo)

HY-078020 (5 mg/kg，灌胃) 抑制 histamine 诱导的 ICR/KM 小鼠皮肤血管舒张和毛细血管通透性，血管通透性抑制率为 58.71 %[1]。
HY-078020 (10 mg/kg，静脉注射) 表现出微弱的抗胆碱能活性，对 wistar 小鼠的唾液分泌抑制率为 10.8%[1]。
HY-078020 在小鼠体内的药代动力学分析[1]：

Pharmacokinetic Analysis of HY-078020 in wistar male rats[1]

route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) Vd (L/kg) CL (mL/h/kg) MRT0-inf(h) F (%)
iv 4 0.653 ± 0.12 - - 1678 ± 152.59 1822.38 ± 224.97 1.77 ± 0.22 37.00 ± 4.62 0.70 ± 0.14 59.55
po 25 4.05 ± 0.81 0.38 ± 0.16 1722.06 ± 337.11 6246.92 ± 1443.28 7209.70 ± 1419.01 21.26 ± 7.42 59.35 ± 10.59 6.01 ± 1.42 -

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

Animal Model: histamine-induced vascular permeability in ICR and Kunming mice[1]
Dosage: 5 mg/kg
Administration: i.g.
Result: Reduced the vascular permeability with an inhibition rate of 58.71%.
Animal Model: Wistar mice[1]
Dosage: 10 mg/kg
Administration: i.v., once a day
Result: Inhibited salivary secretion with an inhibition rate of 10.8%.
分子量

515.09

Formula

C32H35ClN2O2
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

HY-078020 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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:

HY-0780202756222-90-7HY078020HY 078020Histamine ReceptormAChRMuscarinic acetylcholine receptorallergic diseaseanticholinergicantihistamineInhibitorinhibitorinhibit

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产品名称：
HY-078020
目录号：
HY-162231
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