2. GPCR/G Protein
  3. RXFP Receptor
  4. AZ7976

AZ7976 (Compound 42) 是一种针对 Relaxin Family Peptide Receptor 1（RXFP1） 的高选择性激动剂 (pEC50 > 10.5)。该化合物通过别构机制增强 RXFP1 的 cAMP 信号传导，从而在生理上增加了心率。能够用于心血管疾病研究领域。

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AZ7976 Chemical Structure

AZ7976 Chemical Structure

CAS No. : 2813866-27-0

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AZ7976 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

AZ7976 (Compound 42) is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1) (pEC50 > 10.5). AZ7976 enhances RXFP1's cAMP signaling through an allosteric mechanism, thereby physiologically increasing heart rate. AZ7976 can be used in the field of cardiovascular disease research[1].

体外研究
(In Vitro)

AZ7976 (48h) 的细胞毒性分别为 IC50=15 μM (THP1)， 68/37 μM (HepG2 Glu/Gal)，17 μM (HepG2 C3a spheroids)。对于 BSEP，hERG，NaV1.5，KaV4.3 (Ikr) 的抑制作用分别为 IC50 =23 μM (BSEP)，>39 μM (hERG)，231 μM (NaV1.5)，>33 μM (KaV4.3 (Ikr))。在 A549 微核试验中显示遗传毒性为阴性[1]。
AZ7976 (90 min; concentration responses) 在 CHO-hRXFP1 细胞中不与 relaxin H2 竞争结合 RXFP1， 而是增强了 125I-relaxin H2 的结合[1]。
AZ7976 抑制离子通道和 bile salt efflux transporter (BSEP)，对 THP1 具有细胞毒性[1]。

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

AZ7976 相关抗体:
体内研究
(In Vivo)

AZ7976 (i.v.; 初次给药 1.5 mg/kg; i.v.drip; 持续给药 9.0 mg/kg) 导致大鼠心率显著增加，平均动脉血压升高[1]。

药代动力学分析[1]

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

Route Dose (μmol/kg) Vdss (L/kg) Cl (mL/min/kg) t1/2 (h) oral dose (μmol/kg) F (%)
i.v. 0.73 2.3 38 2.9 1.46 11
Animal Model: Sprague-Dawley rats[1]
Dosage: initial 1.5 mg/kg, continuous 9.0 mg/kg
Administration: i.v.; i.v.drip
Result: Caused a significant increase in heart rate and a rise in mean arterial blood pressure in the rats, the same response in Sprague-Dawley rats as after RXFP1 receptor activation
分子量

682.65

Formula

C30H33F7N2O6S
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

AZ7976 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:

AZ79762813866-27-0AZ 7976AZ-7976RXFP ReceptorRXFP1 AgonistCardiovascular EffectsAllosteric ModulationInhibitorinhibitorinhibit

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目录号：
HY-162401
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