KW-8232 free base

Names

[ CAS No. ]:
170365-25-0

[ Name ]:
KW-8232 free base

Biological Activity

[Description]:

KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor
Research Areas >> Metabolic Disease

[Target]

Prostaglandin Receptor[1]


[In Vitro]

KW-8232 free base is an anti-osteoporotic agent. KW-8232 reduces the biosynthesis of PGE2 in mouse osteoblastic cells[1].

[In Vivo]

KW-8232 (3, 10, 30 mg/kg, p.o.) potently increases the femoral bone mineral density (BMD) of immobilized legs of rats, and affects immobilization-induced abnormal bone turnovrer. KW-8232 markedly decreases urinary calcium excreation in the neurectomized rats only at 30 mg/kg, and highly reduces urinary pyridinoline and deoxypyridionline excretion which are markers of bone resorption in neurectomized rats. KW-8232 inhibits bone loss may be attributed to the lower prostaglandins (PGs)-stimulated bone resorption via regulation of PGE2 production[1].

[Animal admin]

After male Sprague-Dawley rats (5-week-old) are anesthetized with sodium pentobarbital (30 mg/kg, i.p.), a dorsolateral incision is made on the right hip through which the sciatic nerve is exposed, and a 0.5-cm section is excised. The contralateral leg is left intact. KW-8232 is dissolved in distilled water and administered orally at 1, 3, 10, and 30 mg/kg once daily beginning 1 day prior to neurectomy. On day 28, rats are exsanguinated under diethyl ether agter obtaining urine, and their femurs are removed. Bone mineral density (BMD) is determined by dual energy x-ray absorptiometry. Twenty-four hour urine samples are collected from the animals, which are fasted immediately after the final administration of KW-8232[1].

[References]

[1]. Uchii M, et al. Effect of KW-8232, a novel anti-osteoporotic agent, on bone loss in sciatic neurectomized rats. Jpn J Pharmacol. 1998 Oct;78(2):241-3.


[Related Small Molecules]

Dinoprostone | Prostaglandin E1 | E7046 | ONO-AE3-208 | PF 04418948 | Fevipiprant | grapiprant | TG6-10-1 | Taprenepag | GW 627368 | MRE-269 | Ramatroban | AH 6809 | Laropiprant | AZD1981

Chemical & Physical Properties

[ Molecular Formula ]:
C36H37ClN4O3

[ Molecular Weight ]:
609.16


Related Compounds