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製品番号: HY-P11619

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R2R01

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₁₉₇H₃₄₄N₄₈O₆₁
分子量:4361.12

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

R2R01 構造式

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

RXFP1

0.34 nM (EC₅₀)

体外実験

R2R01 (30 min) potently activates RXFP1 in OVCAR5 cells with an EC₅₀ of 0.34 ± 0.19 nM in serum-free conditions and 26.5 ± 4.0 nM in the presence of 2% HSA^[1].
R2R01 (30 min) has low mast cell degranulation activity in LAD2 cells, and induces β-hexosaminidase release with EC₅₀ >33 μM^[1].
R2R01 (3 μM; overnight) has a low risk of immunogenicity^[1].

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

体内実験

R2R01 (0.1-1 mg/kg; i.v.; single dose) increases heart rate in pithed rats, with a 40.3 ± 4.7% maximum heart rate increase at 0.3 mg/kg^[1].
R2R01 (0.1-1 mg/kg; s.c.; single dose) produces dose-dependent, long-lasting heart rate increases in conscious telemetered rats^[1].

MedChemExpress (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.

化学情報

分子量 4361.12
分子式 C₁₉₇H₃₄₄N₄₈O₆₁
配列

AC-Leu-Glu-Gly-Arg-Glu-Lys-Val-Arg-Ala-Lys(AC)-Ile-{Aib}-{Aib}-Glu-Gly-Lys{(TTDS)3-γGlu-γGlu-γGlu-C16 acid}-Ser-Thr-Phe-Ser-{Mly}-Arg-Ala-Lys(Ac)-NH2
シーケンスの短縮

Ac-LEGREKVRA-Lys(AC)-I-{Aib}-{Aib}-EG-Lys{(TTDS)3-γGlu-γGlu-γGlu-C16 acid}-STFS-{Mly}-RA-Lys(Ac)-NH2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (264 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Mallart S, et al. Optimization of Single Relaxin B-Chain Peptide Leads to the Identification of R2R01, a Potent, Long-Acting RXFP1 Agonist for Cardiovascular and Renal Diseases. J Med Chem. 2025;68(3):3873-3885. [Content Brief]

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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