Serelaxin (RLX030) is a recombinant form of human relaxin-2 that attenuates cardiac fibrosis by inhibiting endothelial-to-mesenchymal transition through its action on endothelial relaxin family peptide receptor 1 (RXFP1), and may be used in studies related to heart failure.
| Molecular Weight | 5962.95 |
| Formula | C256H408N74O74S8 |
| CAS Number | 99489-94-8 |
| Storage | -20°C |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Marco Metra, et al. N Engl J Med. Effects of Serelaxin in Patients with Acute Heart Failure
[5] Jeremy Tietjens, et al. Heart. Serelaxin and acute heart failure
| Related RXFP Products |
|---|
| CGEN-25010
CGEN-25010 is a relaxin receptor RXFP1/2 agonist that can be used in studies related to cardiovascular disease. |
| AZD5462
AZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, belongs to GPCR family 1c number with anti-fibrotic and anti-inflammatory properties. |
| RLX-33
RLX-33 is a potent and selective blood-brain barrier permeable relaxin family peptide 3 (RXFP3) antagonist that also blocks relaxin 3 (Relaxin 3) -induced ERK1/2 phosphorylation. The IC50 phosphorylated RXFP3, ERK1 and ERK2 were 2.36μM, 7.82μM and 13.86μM, respectively. RLX-33 can block the increase of food intake in rats induced by RXFP3 selective agonist R3/I5. RLX-33 can be used in the study of metabolic syndrome. |
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