标签归档：abaloparatide

Abaloparatide TFA(Synonyms: 阿巴洛肽 BA 058 TFA BIM 44058 TFA)

发表于由

Abaloparatide TFA;(Synonyms: 阿巴洛肽; BA 058 TFA; BIM 44058 TFA) 纯度: 96.11%

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)。

Abaloparatide TFA (Synonyms: 阿巴洛肽; BA 058 TFA; BIM 44058 TFA)

Abaloparatide TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ￥1200 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 询价
200 mg ; 询价 ;
500 mg ; 询价 ;

* Please select Quantity before adding items.

Abaloparatide TFA 相关产品

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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[1][2].

IC50 & Target

Parathyroid hormone receptor 1 (PTHR1)[1]
体外研究
(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)[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.
体内研究
(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[2].

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

Animal Model: Female Sprague-Dawley rats (age 22 weeks)[2]
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%.

Clinical Trial

分子量

4074.61

Formula

C176H301N56F3O51
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
Sequence Shortening

AVSEHQLLHDKGKSIQDLRRRELLEKLL-{Aib}-KLHTA-NH2
中文名称

安巴洛他定； 阿巴洛肽； 阿达帕拉肽
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。
参考文献

  • [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.