2. GPCR/G Protein
  3. Angiotensin Receptor Arrestin
  4. TRV-120027

TRV120027 是血管紧张素 II 受体 1 型 (AT1R) 的 β-arrestin-1 激动剂。TRV120027 通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌，促进质膜上 AT1R-β-arrestin-1-TRPC3-PLCγ 形成大分子复合物。TRV120027 抑制血管紧张素 II 介导的血管收缩并增加心肌细胞的收缩力。TRV120027 有潜力用于急性失代偿性心力衰竭 (ADHF) 的研究。

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TRV-120027 Chemical Structure

TRV-120027 Chemical Structure

CAS No. : 1234510-46-3

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规格 价格 是否有货 数量
1 mg ￥750
In-stock
5 mg ￥2200
In-stock
10 mg ￥3500
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

Other Forms of TRV-120027:

TRV-120027 相关抗体

Top Publications Citing Use of Products

查看 Angiotensin Receptor 亚型特异性产品:

查看所有亚型
AT1 Receptor AT2 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling[1]. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment[2].

IC50 & Target

IC50: the angiotensin II receptor type 1 (AT1R)[1]
体外研究
(In Vitro)

TRV120027 (100 nM) significantly increases the AT1R and TRPC3 association with the immunoprecipitated β-arrestin-1 in HEK293 cells co-transfected with Flag-AT1R-cherry, HA-β-arrestin-1 and TRPC3-GFP[2].
TRV120027 (100 nM) induces an [Ca2+]i increase in HEK293 cells co-transfected with AT1R, β-arrestin-1, and TRPC3, which are significantly blocked by Pyr3 pre-incubation in HEK293 cells co-transfected with Flag-AT1R-Cherry, HA-β-arrestin-1, and TRPC3-GFP[2].

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

TRV-120027 相关抗体:
体内研究
(In Vivo)

TRV120027 (intravenous injection; 0.3 or 1.5 µg/kg per minute; infusion rate, 0.5 mL/min) when added to furosemide decreases cardiac preload and afterload, systemic and renal vascular resistances, and left ventricular external work while increasing cardiac output and renal blood flow. GFR and renal excretory function are maintained in canines with experimental HF[1].

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

Animal Model: Male mongrel dogs (weight, 20.5–30 kg)[1]
Dosage: 0.3 or 1.5 µg/kg per minute; infusion rate, 0.5 mL/min
Administration: Intravenous injection
Result: Resulted in dose-dependent vasodilation, increased cardiac contractility, and decreased myocardial oxygen consumption in dog.
Clinical Trial
分子量

926.07

Formula

C43H67N13O10
CAS 号
性状

固体

颜色

White to off-white

Sequence Shortening

{Sar}-RVYIHPA
运输条件

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

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

溶解性数据
细胞实验： 

H2O 中的溶解度 : 100 mg/mL (107.98 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0798 mL 5.3992 mL 10.7983 mL
5 mM 0.2160 mL 1.0798 mL 2.1597 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

TRV-120027 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.0798 mL 5.3992 mL 10.7983 mL 26.9958 mL
5 mM 0.2160 mL 1.0798 mL 2.1597 mL 5.3992 mL
10 mM 0.1080 mL 0.5399 mL 1.0798 mL 2.6996 mL
15 mM 0.0720 mL 0.3599 mL 0.7199 mL 1.7997 mL
20 mM 0.0540 mL 0.2700 mL 0.5399 mL 1.3498 mL
25 mM 0.0432 mL 0.2160 mL 0.4319 mL 1.0798 mL
30 mM 0.0360 mL 0.1800 mL 0.3599 mL 0.8999 mL
40 mM 0.0270 mL 0.1350 mL 0.2700 mL 0.6749 mL
50 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5399 mL
60 mM 0.0180 mL 0.0900 mL 0.1800 mL 0.4499 mL
80 mM 0.0135 mL 0.0675 mL 0.1350 mL 0.3374 mL
100 mM 0.0108 mL 0.0540 mL 0.1080 mL 0.2700 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

TRV-1200271234510-46-3TRV120027TRV 120027Angiotensin ReceptorArrestinAT1R?acutedecompensatedheartfailureADHF cardiacInhibitorinhibitorinhibit

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