ABALOPARATIDE TFA
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- CAS号:
- 英文名:
- Abaloparatide TFA
- 英文别名:
- BA 058 TFA;BIM 44058 TFA;Abaloparatide TFA;Abaloparatide TFA (247062-33-5 free base)
- 中文名:
- ABALOPARATIDE TFA
- 中文别名:
- 安巴洛他定;ABALOPARATIDE TFA;化合物ABALOPARATIDE TFA (BA 058 TFA)
- CBNumber:
- CB68019750
- 分子式:
- 分子量:
- 0
- MOL File:
- Mol file
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ABALOPARATIDE TFA化学性质
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形态:
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Solid
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颜色:
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White to off-white
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ABALOPARATIDE TFA性质、用途与生产工艺
Abaloparatide TFA (BA 058 TFA) 是一种甲状旁腺激素受体 1 PTHR1 类似物,是 PTHR1 信号通路的有效和选择性激活剂。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)。
Parathyroid hormone receptor 1 (PTHR1)
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
EC
50
value for cAMP formation compared to teriparatide (
EC
50
s 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
EC
50
value for abaloparatide is 1.6-fold lower than that of teriparatide (
EC
50
s 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
EC
50
value of 0.8 nM for Abaloparatide.
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.
Animal Model:
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Female Sprague-Dawley rats (age 22 weeks)
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Dosage:
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1 µg/kg, 5 µg/kg, 25 µg/kg
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Administration:
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Subcutaneous injection; daily; for 12 months
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Result:
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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%.
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ABALOPARATIDE TFA
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ABALOPARATIDE TFA 试剂级价格
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-108742A | ABALOPARATIDE TFA Abaloparatide TFA | | 5mg | 3500元 |
2024/01/25 | HY-108742A | ABALOPARATIDE TFA Abaloparatide TFA | | 1mg | 1200元 |
ABALOPARATIDE TFA 相关搜索:
- 化合物ABALOPARATIDE TFA (BA 058 TFA)
- 安巴洛他定
- ABALOPARATIDE TFA
- BIM 44058 TFA
- BA 058 TFA
- Abaloparatide TFA (247062-33-5 free base)
- Abaloparatide TFA