| Description | Abaloparatide acetate is a parathyroid hormone receptor 1 PTHR1 analogue and an effective and selective activator of the PTHR1 signaling pathway. |
| In vitro | MC3T3-E1成骨细胞在0.5 mM IBMX的存在下，被0.01-100 nM Abaloparatide处理了40分钟，温度为37℃。结果显示，Abaloparatide的暴露显著提高了细胞内cAMP水平。与teriparatide相比，Abaloparatide处理导致cAMP形成的EC50值减少了2.3倍（分别为0.3 nM和0.7 nM）[1]。Abaloparatide呈剂量依赖性地刺激β-arrestin/PTHR1相互作用。相应地，Abaloparatide的EC50值比teriparatide低1.6倍（分别为0.9 nM和1.5 nM）[1]。Abaloparatide有效诱导PTHR1内化的剂量依赖性刺激，最低剂量为0.1 nM，而在100 nM浓度时达到最大刺激。Abaloparatide的EC50值为0.8 nM[1]。 |
| In vivo | Abaloparatide（1-25μg/kg；皮下注射；每日一次；持续12个月；雌性Sprague-Dawley大鼠）治疗能增加生化骨形成标志物，提高松质骨、骨内皮和骨膜表面的组织形态学指标。Abaloparatide显著提高松质骨体积和密度，改善松质骨微结构。它促进胫骨骨干处骨膜的扩张和骨内皮的骨沉积，导致皮质骨体积和密度的显著增加。在骨质疏松的去卵巢(OVX)大鼠中，经过12个月的Abaloparatide（25μg/kg）治疗后，全身骨矿物质密度(BMD)增加了25%[2]。 |
| molecular weight | 4020.71 |
| Molecular formula | C176H304N56O51 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 2.5 mM |
| References | 1. 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. |
Abaloparatide acetate(247062-33-5 free base)
CAS No.:
Abaloparatide acetate is a parathyroid hormone receptor 1 PTHR1 analogue and an effective and selective activator of the
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