2. GPCR/G Protein
  3. Endothelin Receptor
  4. CI-1020

CI-1020 (PD156707) 是一种具有口服活性靶向 endothelin (ETA) 的选择性拮抗剂，其 IC50 为 0.3 nM。 CI-1020 在器官培养中完全阻断人隐静脉内膜增生。CI-1020 抑制缺氧性肺动脉高压并阻断口服给药后ET-1诱导的升压反应。

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CI-1020 Chemical Structure

CI-1020 Chemical Structure

CAS No. : 162256-50-0

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CI-1020 相关抗体

Top Publications Citing Use of Products

查看 Endothelin Receptor 亚型特异性产品:

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ETA ETB

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration[1][2][3].

IC50 & Target[1]

ETA

0.3 nM (IC50)

体外研究
(In Vitro)

CI-1020 (1 μM， 28 天) 在器官培养中完全阻断人隐静脉内膜增生[1]。
CI-1020 (1 μM， 14 天) 对组织无毒[1]。

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

CI-1020 相关抗体:
体内研究
(In Vivo)

CI-1020 (30mg/kg， p.o.) 对 ET-A 完全抑制，并且不影响正常大鼠的基础血压[2]。
CI-1020f (40mg/kg，p.o.) 减轻暴露于慢性缺氧的大鼠中已建立的肺动脉高压[4]。

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

Animal Model: normal rats [2]
Dosage: 30 mg/kg
Administration: oral administration (p.o.)
Result: Inhibited the ET-A and has no significant effect on basal blood pressure in normotensive rats.
Animal Model: basal blood pressure in normotensive rats[4]
Dosage: 40 mg/kg/day
Administration: oral administration (p.o.)
Result: Reduced the increase in RV/LV+S and the percentage DEL induced by chronic hypoxia.
Lowered the increase in pulmonary resistance in isolated perfused lungs significantly.
分子量

506.50

Formula

C28H26O9
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

CI-1020 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:

CI-1020162256-50-0PD156707CI1020CI 1020PD 156707PD-156707Endothelin Receptororally activeselectivehypoxic pulmonary hypertensionInhibitorinhibitorinhibit

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