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  3. Abaloparatide TFA

Abaloparatide TFA (Synonyms: BA 058 TFA; BIM 44058 TFA)

Cat. No.: HY-108742A Purity: 96.08%
Handling Instructions

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Abaloparatide TFA Chemical Structure

Abaloparatide TFA Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1479 In-stock
Estimated Time of Arrival: December 31
1 mg USD 120 In-stock
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5 mg USD 350 In-stock
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10 mg USD 550 In-stock
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25 mg USD 990 In-stock
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50 mg USD 1650 In-stock
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100 mg USD 2250 Get quote
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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]

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].

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].

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%.
Molecular Weight

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
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
Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (12.27 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

AbaloparatideBA 058BIM 44058BA058BA-058BIM44058BIM-44058Thyroid Hormone ReceptorTHRInhibitorinhibitorinhibit

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Abaloparatide TFA
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