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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- Formule: C197H344N48O61
- Masse moléculaire:4361.12
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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RXFP1 0.34 nM (EC50) |
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; 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.
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Animal Model:CD (36-53 weeks old, 435-515 g, conscious telemetered model for RXFP1-mediated chronotropic effect)[1]
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Dosage:0.1, 0.3, 1 mg/kg
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Administration:S.c.; single dose
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Result:Induced dose-dependent and long-lasting increases in heart rate over the 48 h follow-up period.
Chemical Information
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Masse moléculaire 4361.12
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Formule C197H344N48O61
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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
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Sequence Shortening
Ac-LEGREKVRA-Lys(AC)-I-{Aib}-{Aib}-EG-Lys{(TTDS)3-γGlu-γGlu-γGlu-C16 acid}-STFS-{Mly}-RA-Lys(Ac)-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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