产品描述: Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis |
靶点:
Target: Estrogen Receptor;EstrogenReceptor/ERR |
体内研究:
Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels. Lasofoxifene tartrate (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice. Lasofoxifene tartrate (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice |
参考文献:
1. Andersson A, et al. Selective oestrogen receptor modulators lasofoxifene and bazedoxifene inhibit joint inflammation and osteoporosis in ovariectomised mice with collagen-induced arthritis. Rheumatology (Oxford). 2016 Mar;55(3):553-63. 2. Andreano KJ, et al. The Dysregulated Pharmacology of Clinically Relevant ESR1 Mutants is Normalized by Ligand-activated WT Receptor. Mol Cancer Ther. 2020 Jul. 19(7):1395-1405. 3. Lainé M, et al. Lasofoxifene as a potential treatment for therapy-resistant ER-positive metastatic breast cancer. Breast Cancer Res. 2021 May 12. 23(1):54. |
溶解性:
DMSO : 83.33 mg/mL (147.84 mM; Need ultrasonic) |
保存条件:
2-8℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
1.774 ml |
8.871 ml |
17.742 ml |
5 mM |
0.355 ml |
1.774 ml |
3.548 ml |
10 mM |
0.177 ml |
0.887 ml |
1.774 ml |
50 mM |
0.035 ml |
0.177 ml |
0.355 ml |
|
注意: |
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