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Abaloparatide(acetate)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
A synthetic derivative of PTHrP and an agonist of PTHR1
Canonical SMILESCC(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
分子式C174H300N56O49.XC2H4O2
分子量3960.6
溶解度Ethanol: Partially soluble,PBS (pH 7.2): 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Abaloparatide is a synthetic derivative of human parathyroid hormone-related protein (PTHrP) (1-34) and an agonist of parathyroid hormone receptor type 1 (PTH1R).1It 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.2It 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.3Formulations 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)