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Cat. No.: 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.

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화학식: C₁₉₇H₃₄₄N₄₈O₆₁
분자량:4361.12

보관:

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

R2R01 Chemical Structure

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

RXFP1

0.34 nM (EC₅₀)

In Vitro

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.

In Vivo

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.

Chemical Information

분자량 4361.12
화학식 C₁₉₇H₃₄₄N₄₈O₆₁
Sequence

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
Sequence Shortening

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (264 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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