Lasofoxifene (tartrate)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Lasofoxifene (tartrate) is a third-generation, nonsteroidal selective estrogen receptor modulator (SERM).
Estrogen receptors are activated by the hormone estrogen (17β-estradiol). SERMs are characterized by having estrogen agonist action in some tissues while acting as estrogen antagonists in others [1][2].
Lasofoxifene, also known as CP 336,156, is a third-generation, nonsteroidal selective estrogen receptor modulator. Lasofoxifene bound with high affinity to the human estrogen receptor-α with IC50 value of 1.5 nM [1]. Lasofoxifene is also a CB2 inverse agonist [4].
In aged female rats, Lasofoxifene decreased total serum cholesterol and fat body mass, and no uterine hypertrophy was observed. In 5-month-old ovariectomized (OVX) Sprague-Dawley female rats, Lasofoxifene completely prevented OVX-induced increases in body weight gain, total serum cholesterol, and serum osteocalcin. CP-336,156 completely prevented OVX-induced bone loss and inhibited the increased bone turnover associated with estrogen deficiency in lumbar vertebrae, proximal tibiae, and distal femora [1].
In postmenopausal women with osteoporosis, lasofoxifene reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events [2][3].
References:
[1]. Ke HZ, Paralkar VM, Grasser WA, et al. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models. Endocrinology. 1998 Apr;139(4):2068-76.
[2]. Cummings SR, Ensrud K, Delmas PD, et al. Lasofoxifene in postmenopausal women with osteoporosis. N Engl J Med. 2010 Feb 25;362(8):686-96.
[3]. Gennari L, Merlotti D, Nuti R. Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene. Clin Interv Aging. 2010 Feb 2;5:19-29.
[4]. Kumar P, Song ZH. CB2 cannabinoid receptor is a novel target for third-generation selective estrogen receptor modulators bazedoxifene and lasofoxifene. Biochem Biophys Res Commun. 2014 Jan 3;443(1):144-9.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 563.6 |
Cas No. | 190791-29-8 |
Formula | C28H31NO2·C4H6O6 |
Synonyms | CP 336,156 |
Solubility | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide |
Chemical Name | (5R,6S)-5,6,7,8-tetrahydro-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2-naphthalenol, (2S,3S)-2,3-dihydroxybutanedioate |
SDF | Download SDF |
Canonical SMILES | OC(C=C1)=CC2=C1[C@@H](C3=CC=C(OCCN4CCCC4)C=C3)[C@@H](C5=CC=CC=C5)CC2.OC([C@@H](O)[C@H](O)C(O)=O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |