ABALOPARATIDE TFA
- CAS号:
- 英文名:Abaloparatide TFA
- 中文名:ABALOPARATIDE TFA
- CBNumber:CB68019750
- 分子式:
- 分子量:0
- MOL File:Mol file
- 形态 :Solid
- 颜色 :White to off-white
ABALOPARATIDE TFA性质、用途与生产工艺
- 生物活性 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)。
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靶点
Parathyroid hormone receptor 1 (PTHR1)
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体外研究
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. -
体内研究
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: 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%.
- 更新日期:2024/08/19
- 产品编号:HY-108742A
- 产品名称:ABALOPARATIDE TFA Abaloparatide TFA
- CAS编号:
- 包装:1mg
- 价格:1200元
- 更新日期:2024/08/19
- 产品编号:HY-108742A
- 产品名称:ABALOPARATIDE TFA Abaloparatide TFA
- CAS编号:
- 包装:5mg
- 价格:3500元
- 公司名称:天津普西唐生物医药科技有限公司
- 联系电话:010-60605840 15801484223;
- 电子邮件:psaitong@jm-bio.com
- 国家:中国
- 产品数:29778
- 优势度:58
- 公司名称:TargetMol中国(陶术生物)
- 联系电话: 15002134094
- 电子邮件:marketing@targetmol.cn
- 国家:中国
- 产品数:19696
- 优势度:58