BXL-628 is an analog of vitamin D that has diverse biological activities. It increases death of androgen-stimulated human benign prostatic hyperplasia (BPH) cells via induction of apoptosis in a dose-dependent manner. In vivo, BXL-628 completely inhibits androgen-stimulated prostate overgrowth in a rat model of BPH. It reduces expression of IL-13 and IgE/mast cell-derived protease 1 (MMCP1) and decreases edema and leukocyte infiltration in the bladder wall in a mouse model of allergen-induced interstitial cystitis. BXL-628 also reduces the number of adherent endometrial stromal cells and decreases the total weight of endometrial lesions in a mouse model of endometriosis.
BXL-628, a vitamin D analogue, is a selective, orally active vitamin D receptor (VDR) agonist. BXL-628shows anti-inflammatory activity. BXL-628 inhibits growth of prostate cancer cells.
体外研究
BXL-628 (0.00-10 nM; 24-48 hours) can inhibit the proliferation and invasion of DU145 cells.
BXL-628 (10 nM; 8 hours) can inhibit KGFR autophosphorylation and downstream PI3K/AKT activation.
Cell Proliferation Assay
Cell Line:
DU145 cells
Concentration:
0.001 nM, 0.01 nM, 0.1 nM, 1 nM, 10 nM
Incubation Time:
48 hours
Result:
Inhibited dose dependently DU145 cell proliferation with an IC50 of 22.1 pM.
Cell Invasion Assay
Cell Line:
DU145 cells
Concentration:
10 μM
Incubation Time:
24 hours
Result:
Was able to inhibit invasion of DU145 cells.
Western Blot Analysis
Cell Line:
DU145 cells
Concentration:
10 μM
Incubation Time:
8 hours
Result:
Suppressed KGFR autotransphosphorylation and downstream PI3K/AKT activation.
体内研究
BXL-628 (100 μg/kg; oral administration; Once a day; Lasting for 14-28 days, it can inhibit the development of lesions in mouse models of endometriosis and have a protective effect on the implantation and organization of transplanted endometrial tissue.
Animal Model:
Adult Balb/c female mice was induced by injection of syngeneic endometrial tissue fragments.
Dosage:
100 μg/kg
Administration:
p.o.; once a day; for 14-28 days
Result:
Was able to reduce total lesion weight up to 70% upon.
Was shown to reduce the capacity of mouse endometrial cells to adhere to collagen.
Inhibited macrophage recruitment and inflammatory cytokine secretion.
分子式
C29H43FO2
分子量
442.65
CAS号
199798-84-0
中文名称
艾洛骨化醇;2-(甲硫基)噻唑啉
运输条件
Room temperature in continental US; may vary elsewhere.