1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. LGD-3303

LGD-3303 是一种选择性雄激素受体调节剂 (SARM)。

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LGD-3303 Chemical Structure

LGD-3303 Chemical Structure

CAS No. : 917891-35-1

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10 mM * 1 mL in DMSO ¥880
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

LGD-3303 is a selective androgen receptor modulator (SARM).

IC50 & Target

SARM[1]

体外研究
(In Vitro)

LGD-3303 is a nonsteroidal, nonaromatizable androgen receptor ligand that binds to the androgen receptor with high affinity in a radiolabeled to competitive binding assay (Ki=0.9 nM). LGD-3303 binds to the mineralocorticoid, glucocorticoid, and progesterone receptors with greatly reduces affinity in comparison with the androgen receptor (Ki=1261, 581, and 136 nM, respectively). LGD-3303 potently activates transcription through the androgen receptor (EC50=3.6 nM) and has 134% efficacy relative to the steroidal androgen Dihydrotestosterone (DHT)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

LGD-3303 completely inhibits the loss of muscle weight with an oral dose of 1 mg/kg/day. At higher doses, LGD-3303 significantly increases levator ani muscle weight above eugonadal levels. In contrast, LGD-3303 has greatly reduced potency and efficacy on the other measured endpoints. LGD-3303 does not maintain eugonadal levels of serum LH at doses less than 10 mg/kg/day. LGD-3303 maintains eugonadal prostate weight only at doses of 100 mg/kg/day or greater and never fully returns the mean preputial gland weight to eugonadal levels at any tested dos. In no case does LGD-3303 restore LH, prostate, or preputial gland weights to supraphysiological levels significantly exceeding sham-operated controls. The ventral prostate, in particular, demonstrates a greatly reduced response to LGD-3303. At the muscle normalizing dose (1 mg/kg/day), ventral prostate weight is not significantly increased above the level of ORDX control rats (20% efficacy relative to intact rats). At the highest doses tested, ventral prostate never significantly exceeds eugonadal levels and reaches an apparent plateau with minimal increase in prostate weight as dosing escalated from 30 to 300 mg/kg/day. To investigate this apparent plateau in pharmacological activity, plasma concentrations of LGD-3303 are analyzed from the highest dose groups. Exposure to LGD-3303 (AUC0-6) monotonically increases with dose from 10 to 300 mg/kg/day[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

342.74

Formula

C16H14ClF3N2O

CAS 号
性状

固体

颜色

Light yellow to yellow

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
细胞实验: 

DMSO 中的溶解度 : 10.42 mg/mL (30.40 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9177 mL 14.5883 mL 29.1766 mL
5 mM 0.5835 mL 2.9177 mL 5.8353 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

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

    Solubility: 1.67 mg/mL (4.87 mM); 悬浊液; 超声助溶

    此方案可获得 1.67 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 16.7 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。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

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

    Solubility: 1.04 mg/mL (3.03 mM); 悬浊液; 超声助溶

    此方案可获得 1.04 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 10.4 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.57%

参考文献
Kinase Assay
[1]

In vitro binding is determined using recombinant baculovirus expressed human androgen receptor (hAR), human glucocorticoid receptor (hGR), human mineralocorticoid receptor (hMR), or human progesterone receptor (hPR). Tritium-labeled reference ligand is used with varying concentrations of LGD-3303 as a competing ligand. Inhibition constant (Ki) values are calculated by application of the Cheng-Prusoff equation. Reporter assays are performed. Briefly, CV1 cells are cultured in DMEM supplemented with 10% charcoal resin-stripped fetal bovine serum (FBS), and seeded 48 h before transfection in 96-well microtiter plates. Cells are transiently transfected using a nonliposomal formulation, the FuGENE 6 transfection reagent, with luciferase reporter plasmids MMTV-LUC or MTV-ERE5-LUC, a β-galactosidase (β-Gal) expression plasmid coding for the constitutive expression of Escherichia coli β-galactosidase, and hAR, hGR, hMR, hPR, or human estrogen receptor α (pRShERα) expression plasmids. Cells are treated with varying concentrations of LGD-3303 or reference compound for 40 h. The normalized luciferase response is calculated as relative luciferase units/(β-gal O.D415/β-Gal incubation time in minutes). The effective concentration that produces 50% of the maximum response (EC50) is determined, and agonist efficacy is calculated as a percent of normalized luciferase response relative to the maximum response by the reference agonist (i.e., DHT for hAR, dexamethasone for hGR, aldosterone for hMR, progesterone for hPR-B, or 17β-estradiol for hERα)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Rats[2]
Male Sprague-Dawley rats (7-8 weeks old, 200 g) are used. Rats are sorted by weight, assigned to experimental groups (n=5/group), and surgery is performed. Experimental groups consist of LGD-3303 (doses ranged from 0.1-300 mg/kg/day) or vehicle. LGD-3303 is administered by once daily oral gavage in a volume of 4 mL/kg. On the 14th day, blood is collected into lithium heparin tubes by jugular puncture at 0, 0.5, 1, 2, 4, and 6 h postdosing from the animals in the high-dose groups. Blood is centrifuged, and plasma is stored at -20°C for pharmacokinetic analysis. On the 15th day, rats are killed by decapitation, and trunk blood is collected, allowed to clot in serum separator tubes, and centrifuged, and serum is stored at -80°C for future analysis of serum luteinizing hormone (LH) levels. The wet weights of the ventral prostate, levator ani muscle, and preputial gland are measured at necropsy[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9177 mL 14.5883 mL 29.1766 mL 72.9416 mL
5 mM 0.5835 mL 2.9177 mL 5.8353 mL 14.5883 mL
10 mM 0.2918 mL 1.4588 mL 2.9177 mL 7.2942 mL
15 mM 0.1945 mL 0.9726 mL 1.9451 mL 4.8628 mL
20 mM 0.1459 mL 0.7294 mL 1.4588 mL 3.6471 mL
25 mM 0.1167 mL 0.5835 mL 1.1671 mL 2.9177 mL
30 mM 0.0973 mL 0.4863 mL 0.9726 mL 2.4314 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LGD-3303
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HY-103576
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