Abaloparatide (acetate) (Synonyms: BA 058, BIM 44058) |
| カタログ番号GC46768 |
PTHrPの合成誘導体であり、PTHR1のアゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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Abaloparatide is a synthetic derivative of human parathyroid hormone-related protein (PTHrP) (1-34) and an agonist of parathyroid hormone receptor type 1 (PTH1R).1 It selectively binds to the G protein-dependent (RG) conformation of PTH1R over the G protein-independent (R0) conformation (IC50s = 0.2 and 316.23 nM, respectively). It induces cAMP signaling more transiently than PTH (1-34) , PTHrP (1-36), or the long-acting PTH/PTHrP hybrid peptide analog LA-PTH (EC50s = 0.08, 0.44, 0.46, and 0.21 nM, respectively). Abaloparatide (5 and 20 µg/kg per day for six weeks) increases areal bone mineral density in the lumbar spine, total femur, and femur diaphysis in ovariectomized osteopenic rats.2 It also increases bone strength in the femur diaphysis, femur neck, and L4 vertebra in the same model. Abaloparatide increases the incidence of focal osteoblast hyperplasia, benign osteoblastoma, and osteosarcoma in rats in a time- and dose-dependent manner when administered at doses greater than or equal to 10 µg/kg per day for up to two years.3 Formulations containing abaloparatide have been used in the treatment of osteoporosis in postmenopausal women at high risk for bone fracture.
1.Hattersley, G., Dean, T., Corbin, B.A., et al.Binding selectivity of abaloparatide for PTH-type-1-receptor conformations and effects on downstream signalingEndocrinology157(1)141-149(2016) 2.Bahar, H., Gallacher, K., Downall, J., et al.Six weeks of daily abaloparatide treatment increased vertebral and femoral bone mineral density, microarchitecture and strength in ovariectomized osteopenic ratsCalcif. Tissue Int.99(5)489-499(2016) 3.Jolette, J., Attalla, B., Varela, A., et al.Comparing the incidence of bone tumors in rats chronically exposed to the selective PTH type 1 receptor agonist abaloparatide or PTH(1-34)Regul. Toxicol. Pharmacol.86356-365(2017)
| Cas No. | N/A | SDF | |
| 同義語 | BA 058, BIM 44058 | ||
| Canonical SMILES | CC(O)=O.C[C@@H](C(N)=O)NC([C@H]([C@H](O)C)NC([C@H](CC1=CNC=N1)NC([C@H](CC(C)C)NC([C@H](CCCCN)NC(C(C)(C)NC([C@H](CC(C)C)NC([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](CC2=CNC=N2)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@H](CCC(N)=O)NC([C@H](CC3=CNC=N3)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)=O)=O)=O)=O)=O)=O)=O | ||
| Formula | C174H300N56O49.XC2H4O2 | M.Wt | 3960.6 |
| 溶解度 | Ethanol: Partially soluble,PBS (pH 7.2): 10 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.2525 mL | 1.2624 mL | 2.5249 mL |
| 5 mM | 0.0505 mL | 0.2525 mL | 0.505 mL |
| 10 mM | 0.0252 mL | 0.1262 mL | 0.2525 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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