产品
编 号:F291227
分子式:C174H300N56O49
分子量:3960.59
产品类型
结构图
CAS No: 247062-33-5
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产品详情
生物活性:
Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis.
体内研究:
Abaloparatide (20-80 μg/kg; s.c.; daily for 30 days) enhances bone formation and cortical structure in mouse.Animal Model:16-week-old wild-type (WT) female C57BL/6J mice
Dosage:20-80 μg/kg
Administration:S.c.; daily for 30 days
Result:Efficiently expanded cortical thickness (Ct. Th) at both doses of 20 and 80 μg/kg/day by 17% and 18%, respectively, increased P1NP levels to 227% and 407% at 20 and 80 μg/kg/day, respectively.
Animal Model:Female Sprague-Dawley rats (age 22 weeks)
Dosage:1 μg/kg, 5 μg/kg, 25 μg/kg
Administration:Subcutaneous injection; daily; for 12 months
Result:Increased biochemical bone formation markers, histomorphometric indices of bone formation on trabecular, endocortical, and periosteal surfaces. Induced substantial increases in trabecular bone volume and density and improvements in trabecular microarchitecture. Stimulated periosteal expansion and endocortical bone apposition at the tibial diaphysis, leading to marked increases in cortical bone volume and density. Whole-body bone mineral density (BMD) was increasing 25%.
体外研究:
Abaloparatide (0-100 nM; 40 min) enhances Gs/cAMP signaling and β-arrestin recruitment in MC3T3-E1 cells.Abaloparatide (0-100 nM) efficiently induces PTHR1 internalization in a dose-dependen manner with an EC50 value of 0.8 nM in U2OS Cell.