Abaloparatide TFA - KKL Med Inc.

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Abaloparatide TFA

目录号 : KM4599 纯度 : 96%

Data Sheet 产品使用指南

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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5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

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.

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 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.

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%.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Protect from light, stored under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

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

溶解性数据

In Vitro:

H₂O : ≥ 50 mg/mL (12.27 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.2454 mL	1.2271 mL	2.4542 mL
5 mM	0.0491 mL	0.2454 mL	0.4908 mL
10 mM	0.0245 mL	0.1227 mL	0.2454 mL

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。

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