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RXFP2 agonist 2 is a selective, orally active and allosteric RXFP2 agonist with an EC50 value of 0.38 μM. RXFP2 agonist 2 induces osteoblast mineralization. RXFP2 agonist 2 increases bone formation in female mice. RXFP2 agonist 2 has the potential for the research of osteoporosis[1]. | [in vivo]
RXFP2 agonist 2 (10 mg/kg; p.o.; 3 times per week for 8 weeks) promotes bone formation in female mice[1]. | Animal Model: | 8-week-old WT C57BL/6?J female mice[1] | | Dosage: | 3 mg/kg for i.v.; 10 mg/kg for p.o. | | Administration: | I.v. or p.o. | | Result: | Exhibited a half-life of between 4-6.5?h depending on the route of administration, with no accumulation at 10?mg/kg, and oral bioavailability around 25-31%. |
| Animal Model: | 8-week-old WT C57BL/6?J female mice[1] | | Dosage: | 10 mg/kg | | Administration: | P.o.; 3 times per week for 8 weeks | | Result: | Increased bone formation in mouse with significantly increased in Tb.N and Tb.Th, and increased BV/TV and decreased Tb.Sp. |
| [References]
[1] Esteban-Lopez M, et al. Discovery of small molecule agonists of the Relaxin Family Peptide Receptor 2. Commun Biol. 2022 Nov 4;5(1):1183. DOI:10.1038/s42003-022-04143-9 |
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