Formulation: A solid
Formal Name: L-alanyl-L-valyl-L-seryl-L-α-glutamyl-L-histidyl-L-glutaminyl-L-leucyl-L-leucyl-L-histidyl-L-α-aspartyl-L-lysylglycyl-L-lysyl-L-seryl-L-isoleucyl-L-glutaminyl-L-α-aspartyl-L-leucyl-L-arginyl-L-arginyl-L-arginyl-L-α-glutamyl-L-leucyl-L-leucyl-L-α-glutamyl-L-lysyl-L-leucyl-L-leucyl-2-methylalanyl-L-lysyl-L-leucyl-L-histidyl-L-threonyl-L-alaninamide, acetate
Purity: ≥95%
Formula Markup: C174H300N56O49 • XC2H4O2
Formula Weight: 3960,6
Shelf life (days): 1460
Notes: Abaloparatide is a synthetic derivative of human parathyroid hormone-related protein (PTHrP) (1-34) and an agonist of parathyroid hormone receptor type 1 (PTH1R).{47774} It selectively binds to the G protein-dependent (RG) conformation of PTH1R over the G protein-independent (R0) conformation (IC50s = 0.2 and 316.23 nM, respectively). It induces cAMP signaling more transiently than PTH (1-34) (Item No. 24985), PTHrP (1-36), or the long-acting PTH/PTHrP hybrid peptide analog LA-PTH (EC50s = 0.08, 0.44, 0.46, and 0.21 nM, respectively). Abaloparatide (5 and 20 µg/kg per day for six weeks) increases areal bone mineral density in the lumbar spine, total femur, and femur diaphysis in ovariectomized osteopenic rats.{47775} It also increases bone strength in the femur diaphysis, femur neck, and L4 vertebra in the same model. Abaloparatide increases the incidence of focal osteoblast hyperplasia, benign osteoblastoma, and osteosarcoma in rats in a time- and dose-dependent manner when administered at doses greater than or equal to 10 µg/kg per day for up to two years.{47776} Formulations containing abaloparatide have been used in the treatment of osteoporosis in postmenopausal women at high risk for bone fracture.
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