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^[1].

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.

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.

4361.12

C₁₉₇H₃₄₄N₄₈O₆₁

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

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

Room temperature in continental US; may vary elsewhere.

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

• [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]