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AZD2858

Cat. No. M2178
AZD2858 Structure
Size Price Availability Quantity
10mg USD 125 In stock
50mg USD 445 In stock
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Biological Activity

AZD2858 is a potent orally active glycogen synthase kinase 3 (GSK-3) inhibitor. AZD2858 exposure increased the bone formation biomarker P1NP, and reduced the resorption biomarker TRAcP-5b, indicating increased bone anabolism and reduced resorption in rats. AZD2858 caused β-catenin stabilisation in human and rat mesenchymal stem cells, stimulated hADSC commitment towards osteoblasts and osteogenic mineralisation in vitro. Treatment (1 μM) of human osteoblast cells with AZD2858 in vitro increased β-catenin levels after a short period of time. In rats, oral AZD2858 treatment caused a dose-dependent increase in trabecular bone mass compared to control after a two-week treatment with a maximum effect at a dose of 20 mg/kg once daily (total BMC: 172% of control; p<0.001).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 453.52
Formula C21H23N7O3S
CAS Number 486424-20-8
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

Human stem cell osteoblastogenesis mediated by novel glycogen synthase kinase 3 inhibitors induces bone formation and a unique bone turnover biomarker profile in rats.
Gilmour PS, et al. Toxicol Appl Pharmacol. 2013 Jul 18;272(2):399-407. PMID: 23872097.

Rats treated with AZD2858, a GSK3 inhibitor, heal fractures rapidly without endochondral bone formation.
Sisask G, et al. Bone. 2013 May;54(1):126-32. PMID: 23337038.

GSK-3 inhibition by an orally active small molecule increases bone mass in rats.
Marsell R, et al. Bone. 2012 Mar;50(3):619-27. PMID: 22142634.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD2858 supplier, GSK-3, inhibitors

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