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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C197H344N48O61
- Molecular Weight:4361.12
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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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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Molecular Weight 4361.12
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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