[CAS NO. ] Abaloparatide TFA

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PRODUCTS SPECIFICATIONS

Catalog

HY-108742A

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	4074.61
Molecular Formula	C176H301N56F3O51
SMILES	-

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

1 Publications Citing Use of MCE

[1]Proc Natl Acad Sci U S A. 2021 Nov 9;118(45):e2107363118.

Summary

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 ( EC ₅₀ of 0.3 nM) and β-arrestin recruitment ( EC ₅₀ 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 EC ₅₀ value for cAMP formation compared to teriparatide ( EC ₅₀ s 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 EC ₅₀ value for abaloparatide is 1.6-fold lower than that of teriparatide ( EC ₅₀ s 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 EC ₅₀ value of 0.8 nM for Abaloparatide ^[1] .

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

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04167163	University of Wisconsin, Madison\|Radius Health, Inc.	Osteoporosis\|Arthroplasties, Knee Replacement	January 10, 2020	Phase 4
NCT03746041	University of Rochester	Myelodysplastic Syndromes\|Chronic Myelomonocytic Leukemia	February 14, 2019	Phase 1
NCT03710889	Radius Health, Inc.	Osteoporosis, Postmenopausal\|Osteoporosis\|Osteoporosis Vertebral\|Osteoporosis Risk\|Osteoporosis Fracture\|Osteoporosis Localized to Spine\|Osteoporosis, Age-Related\|Osteoporosis Senile\|Osteoporosis of Vertebrae	September 20, 2018	Phase 3
NCT04760782	David Lunardini\|University of Vermont	Odontoid Fracture	May 18, 2022	Phase 2
NCT04974723	Radius Health, Inc.\|PRA Health Sciences	Osteoporosis, Postmenopausal	July 1, 2021
NCT01674621	Radius Health, Inc.\|Nordic Bioscience A+S	Post Menopausal Osteoporosis	September 25, 2012	Phase 2
NCT04467983	Felicia Cosman, MD\|Crozer-Keystone Health System\|Radius Health, Inc.\|Osteoporosis Center of Delaware County	Osteoporosis, Postmenopausal	February 1, 2021	Phase 4
NCT04249232	Hospital for Special Surgery, New York\|Weill Medical College of Cornell University\|Icahn School of Medicine at Mount Sinai\|New York University\|Westchester Medical Center	Fracture of Pelvis (Disorder)	September 17, 2020	Phase 2
NCT04064411	Radius Health, Inc.	Postmenopausal Osteoporosis	August 5, 2019	Phase 3
NCT03841058	Hospital for Special Surgery, New York	Spinal Fusion	August 14, 2019	Phase 2
NCT03512262	Radius Health, Inc.	Osteoporosis\|Osteoporosis, Age-Related\|Osteoporosis Localized to Spine\|Age Related Osteoporosis\|Osteoporosis Senile\|Osteoporosis of Vertebrae	March 30, 2018	Phase 3
NCT03708926	Johns Hopkins University	Degeneration Disc Intervertebral	March 2021	Phase 2
NCT04626141	Daniel Horwitz\|Radius Health, Inc.\|Geisinger Clinic	Femoral Fractures	July 2022	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

Solvent & Solubility

In Vitro:

H ₂ O : ≥ 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.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 20 mg/mL (4.91 mM); Clear solution; Need ultrasonic and warming

* All of the co-solvents are available by MCE.