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Purity: ≥98%
Abaloparatide (Trade name Tymlos; formerly known as BA-058; ITM-058; BIM 44058) is a 34 amino acid synthetic analog of parathyroid hormone-related protein (PTHrP) that is used to treat osteoporosis. The Food and Drug Administration (FDA) approved it on April 28, 2017, for the treatment of postmenopausal osteoporosis. Not unlike bisphosphonates, but similar to the related medication teriparatide, it is an anabolic (bone-growing) agent. The drug's subcutaneous injection formulation has finished a Phase III osteoporosis trial. Only this one study revealed a decline in fractures. Parathyroid hormone (PTH) (1-34) and parathyroid hormone-related protein (PTHrP) (1-34) share 76% and 41% homology, respectively, with abaloparatide. By selectively activating the parathyroid hormone 1 receptor (PTH1R), a G protein-coupled receptor (GPCR) expressed in osteoblasts and osteocytes, it functions as an anabolic agent for bone. Abaloparatide preferentially binds the PTH1R's RG conformational state, which causes a brief downstream cyclic AMP signaling response that points in the direction of a more anabolic signaling pathway.
| ln Vitro |
Abaloparatide (0-100 nM; 40 min) increases β-arrestin recruitment and Gs/cAMP signaling in MC3T3-E1 cells[1].
Abaloparatide (0-100 nM) effectively and dose-dependently induces PTHR1 internalization in U2OS cells, with an EC50 value of 0.8 nM[1]. |
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| ln Vivo |
In mice, abelaparatide (20–80 µg/kg; s.c.; daily for 30 days) improves cortical structure and bone formation[1].
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| Animal Protocol |
16-week-old wild-type (WT) female C57BL/6J mice[1]
20-80 µg/kg S.c.; daily for 30 days |
| References |
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| Molecular Formula |
C174H299N56O49
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|---|---|
| Molecular Weight |
3959.65
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| Elemental Analysis |
C, 52.58; H, 7.62; N, 19.51; O, 20.29
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| CAS # |
247062-33-5
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| Related CAS # |
Abaloparatide TFA
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| Appearance |
Solid powder
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| SMILES |
O=C([C@H](CC(C)C)NC([C@H](CCCCN)NC([C@H](CCC(=O)O)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@H](CCC(=O)O)NC([C@H](CCCNC(=N)N)NC([C@H](CCCNC(=N)N)NC([C@H](CCCNC(=N)N)NC([C@H](CC(C)C)NC([C@H](CC(=O)O)NC([C@H](CCC(N)=O)NC([C@H]([C@@H](C)CC)NC([C@H](CO)NC([C@H](CCCCN)NC(CNC([C@H](CCCCN)NC([C@H](CC(=O)O)NC([C@H](CC1=CN=CN1)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@H](CCC(N)=O)NC([C@H](CC1=CN=CN1)NC([C@H](CCC(=O)O)NC([C@H](CO)NC([C@H](C(C)C)NC([C@H](C)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)N[C@H](C(NC(C)(C)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)C)=O)[C@@H](C)O)=O)CC1=CN=CN1)=O)CC(C)C)=O)CCCCN)=O)=O)CC(C)C
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| Chemical Name |
Ala-Val-Ser-Glu-His-Gln-Leu-Leu-His-Asp-Lys-Gly-Lys-Ser-Ile-Gln-Asp-Leu-Arg-ArgArg-Glu-Leu-Leu-Glu-Lys-Leu-Leu-Aib-Lys-Leu-His-Thr-Ala-NH2
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| Synonyms |
BIM-44058; Abaloparatide acetate; BA-058; ITM-058; BIM 44058; BA 058;ITM 058; BIM44058; BA058;ITM058; trade name: Tymlos
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (0.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (0.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (0.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2525 mL | 1.2627 mL | 2.5255 mL | |
| 5 mM | 0.0505 mL | 0.2525 mL | 0.5051 mL | |
| 10 mM | 0.0253 mL | 0.1263 mL | 0.2525 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03841058 | Recruiting | Drug: Abaloparatide Drug: Placebo |
Spinal Fusion | Hospital for Special Surgery, New York |
August 14, 2019 | Phase 2 |
| NCT04626141 | Not yet recruiting | Drug: Abaloparatide Drug: Placebo |
Femoral Fractures | Daniel Horwitz | September 2023 | Phase 4 |
| NCT04167163 | Recruiting | Drug: Abaloparatide | Osteoporosis Arthroplasties, Knee Replacement |
University of Wisconsin, Madison | January 10, 2020 | Phase 4 |
| NCT04760782 | Recruiting | Drug: Abaloparatide Device: Hard collar immobilization |
Odontoid Fracture | David Lunardini | May 18, 2022 | Phase 2 |
| NCT03710889 | Completed | Drug: Abaloparatide | Osteoporosis Osteoporosis Risk |
Radius Health, Inc. | September 20, 2018 | Phase 3 |
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