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Abaloparatide TFA

CAS No. :

MCE 站：Abaloparatide TFA

产品活性：Abaloparatide TFA (BA 058 TFA) 是一种甲状旁腺激素受体 1 PTHR1 类似物，是 PTHR1 信号通路的选择性激活剂。Abaloparatide TFA 增强 MC3T3-E1 成骨细胞的 Gs/cAMP 信号传导 (EC₅₀ 为 0.3 nM) 和 β-arrestin 的募集 (EC₅₀ 为 0.9 nM)。

研究领域：Others

作用靶点：Thyroid Hormone Receptor

In Vitro: MC3T3-E1 osteoblast cells are treated with 0.01-100 nM of Abaloparatide for 40 min at 37 ℃ in the presence of 0.5 mM IBMX. The results reveals that exposure of cells to Abaloparatide caused a robust elevation of intracellular cAMP levels. Abaloparatide treatment results in a 2.3-fold decrease in EC₅₀ value for cAMP formation compared to teriparatide (EC₅₀s of 0.3 nM ａnd 0.7 nM, respectively).
A dose-dependent stimulation of β-arrestin/PTHR1 interaction is demonstrated by abaloparatide. Consistently, the calculates the EC₅₀ value for abaloparatide is 1.6-fold lower than that of teriparatide (EC₅₀s of 0.9 nM ａnd 1.5 nM, respectively).
Abaloparatide efficiently induces a dose-dependent stimulation of PTHR1 internalization with a dose as low as 0.1 nM ａnd reaches maximum stimulation at 100 nM concentration. The EC₅₀ value of 0.8 nM for Abaloparatide.

In Vivo: Abaloparatide (1-25 µg/kg; subcutaneous injection; daily; for 12 months; female Sprague-Dawley rats) treatment increases biochemical bone formation markers, histomorphometric indices of bone formation on trabecular, endocortical, ａnd periosteal surfaces. Abaloparatide induces substantial increases in trabecular bone volume ａnd density ａnd improvements in trabecular microarchitecture. Abaloparatide stimulates 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) is increasing 25% after 12 months of abaloparatide (25 μg/kg) in osteopenic ovariectomized (OVX) rats.

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