1. GPCR/G Protein
  2. RXFP Receptor
  3. R2R01

R2R01 是一种强效且选择性的松弛素家族肽受体 1 (RXFP1) 激动剂,其 EC50 值为 0.34 nM。R2R01 可激活 RXFP1 以诱导类松弛素的生物学应答。R2R01 能提高去神经支配大鼠和清醒大鼠的心率。R2R01 可用于心血管疾病的相关研究。

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Custom Peptide Synthesis

R2R01

R2R01 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

R2R01 is a potent and selective relaxin family peptide receptor 1 (RXFP1) agonist with an EC50 of 0.34 nM. R2R01 activates RXFP1 to induce relaxin-like biological responses. R2R01 can increase heart rate in pithed and conscious rats. R2R01 can be used for the research of cardiovascular diseases[1].

IC50 & Target[1]

RXFP1

0.34 nM (EC50)

体外研究
(In Vitro)

R2R01 (30 min) 可在 OVCAR5 细胞中强效激活 RXFP1,在无血清条件下其 EC50 为 0.34 ± 0.19 nM,在含 2% HSA 的条件下则为 26.5 ± 4.0 nM[1]
R2R01 (30 min) 在 LAD2 细胞中具有较低的肥大细胞脱颗粒活性,诱导 β- 己糖胺酶释放的 EC50 值大于 33 μM[1]
R2R01 (3 μM;孵育过夜) 具有较低的免疫原性风险[1]

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

体内研究
(In Vivo)

R2R01 (0.1-1 mg/kg; 静脉注射.; 单次给药) 增加去神经支配大鼠的心率,其在 0.3 mg/kg 时最大心率提升幅度为 40.3 ± 4.7%[1]
R2R01 (0.1-1 mg/kg;皮下注射;单次给药) 可在植入遥测设备的清醒大鼠中产生剂量依赖性、持续时间较长的心率升高[1]

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

Animal Model: CD (36-53 weeks old, 435-515 g, conscious telemetered model for RXFP1-mediated chronotropic effect)[1]
Dosage: 0.1, 0.3, 1 mg/kg
Administration: S.c.; single dose
Result: Induced dose-dependent and long-lasting increases in heart rate over the 48 h follow-up period.
分子量

4361.12

Formula

C197H344N48O61

Sequence

AC-Leu-Glu-Gly-Arg-Glu-Lys-Val-Arg-Ala-Lys(AC)-Ile-{Aib}-{Aib}-Glu-Gly-Lys(PEG6-γGlu-γGlu-γGlu-C16 acid)-Ser-Thr-Phe-Ser-{Mly}-Arg-Ala-Lys(Ac)-NH2

Sequence Shortening

Ac-LEGREKVRA-Lys(AC)-I-{Aib}-{Aib}-EG-Lys(PEG6-γGlu-γGlu-γGlu-C16 acid)-STFS-{Mly}-RA-Lys(Ac)-NH2

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
  • 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.

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R2R01
目录号:
HY-P11619
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