Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue selected to be a potent and selective activator of the PTHR1 signaling pathway. Abaloparatide TFA enhances Gs/cAMP signaling (EC₅₀ of 0.3 nM) and β-arrestin recruitment (EC₅₀ of 0.9 nM) in MC3T3-E1 osteoblast cells^[1][2].

Parathyroid hormone receptor 1 (PTHR1)^[1]

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)^[1].
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)^[1].
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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

4074.61

C₁₇₆H₃₀₁N₅₆F₃O₅₁

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

AVSEHQLLHDKGKSIQDLRRRELLEKLL-{Aib}-KLHTA-NH2

安巴洛他定； 阿巴洛肽； 阿达帕拉肽

Room temperature in continental US; may vary elsewhere.

Protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

H₂O : ≥ 50 mg/mL (12.27 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

• [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.

  [2]. Varela A, et al. One Year of Abaloparatide, a Selective Activator of the PTH1 Receptor, Increased Bone Formation and Bone Mass in Osteopenic Ovariectomized Rats Without Increasing Bone Resorption. J Bone Miner Res. 2017 Jan;32(1):24-33.