Lasofoxifene - CAS:180916-16-9

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Lasofoxifene (Synonyms:拉索昔芬; CP-336156)

目录号 : KCM12092 CAS No. : 180916-16-9 纯度 : ≥98%

Data Sheet 产品使用指南

Lasofoxifene is a third-generation, non-steroidal selective estrogen receptor modulator (SERM). It selectively binds to human ERα with an IC value of 1.5 nM and inhibits bone loss in ovariectomized rats. In clinical studies of postmenopausal osteoporosis, 0.5 mg/day lasofoxifene was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events. Lasofoxifene has also been shown to act as an inverse agonist at the CB cannabinoid receptor, indicating its potential to be repurposed as a therapeutic for indications wherein CB is a target.

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

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生物活性

Lasofoxifene is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis.

体外研究

Lasofoxifene (1 nM-1 μM; 48 h) shows antagonist activity on ER+ breast cancer cells without being affected by the expression level of activating ERα mutants relative to wild-type (WT) ERα.

体内研究

Lasofoxifene (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 in mice.
Lasofoxifene (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 (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.

Animal Model:	Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated)
Dosage:	4 mg/mouse/day
Administration:	Subcutaneous injection; 5 days a week from the first signs of arthritis (day 18); 43 days
Result:	Reduced in arthritis severity, including synovial inflammation and destruction of joints reduction. The mean arthritis frequency was 47% while the vehicle group was 81% at 42 days post immunization.

Animal Model:	NSG mices with xenograft tumors model (MIND, mammary intraductal): WT, Y537S and D538G ERα render tumors
Dosage:	1, 5, or 10 mg/kg
Administration:	Subcutaneous injection; 5 days per week; for 70 days
Result:	Elicited a superior inhibitory effect at a dose of 10 mg/kg, resulted potential tumor shrinkage in Y537S and D538G tumors. And also reduced tumor weight to 60% for Y537S and 50% for D538G at 5 and 10 mg/kg, respectively.

分子式

C₂₈H₃₁NO₂

分子量

413.55

CAS号

180916-16-9

中文名称

拉索昔芬

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 9.09 mg/mL (21.98 mM; ultrasonic and adjust pH to 4 with 1 M HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4181 mL	12.0904 mL	24.1809 mL
5 mM	0.4836 mL	2.4181 mL	4.8362 mL
10 mM	0.2418 mL	1.2090 mL	2.4181 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 1.82 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 1.82 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 18.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.82 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 1.82 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 18.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 1.82 mg/mL (4.40 mM); Clear solution

此方案可获得 ≥ 1.82 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 18.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥98%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器