Abaloparatide TFA (247062-33-5 free base)
CAS No. ——
Abaloparatide TFA (247062-33-5 free base) ( BA 058 TFA; BIM 44058 TFA )
产品货号. M29914 CAS No. ——
Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 PTHR1 analogue and an effective and selective activator of the PTHR1 signaling pathway.
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
规格 | 价格/人民币 | 库存 | 数量 |
100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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生物学信息
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产品名称Abaloparatide TFA (247062-33-5 free base)
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 PTHR1 analogue and an effective and selective activator of the PTHR1 signaling pathway.
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产品描述Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 PTHR1 analogue and an effective and selective activator of the PTHR1 signaling pathway.(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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同义词BA 058 TFA; BIM 44058 TFA
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通路Others
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靶点Other Targets
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受体Parathyroid hormone receptor 1 (PTHR1)
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研究领域——
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适应症——
化学信息
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CAS Number——
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分子量4074.6
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分子式C176H301N56F3O51
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纯度>98% (HPLC)
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溶解度H2O : ≥ 50 mg/mL (12.27 mM)
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SMILES——
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化学全称Sequence:Ala-Val-Ser-Glu-His-Gln-Leu-Leu-His-Asp-Lys-Gly-Lys-Ser-Ile-Gln-Asp-Leu-Arg-Arg-Arg-Glu-Leu-Leu-Glu-Lys-Leu-Leu-{Aib}-Lys-Leu-His-Thr-Ala-NH2
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
Sahbani K, et al. Abaloparatide exhibits greater osteoanabolic response and higher cAMP stimulation and β-arrestin recruitment than teriparatide. Physiol Rep. 2019 Oct;7(19):e14225.
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