AL 082D06 (Synonyms:D06; D-06)
目录号 : KM7148 CAS No. : 256925-03-8 纯度 : 98%

AL 082D06 是一种选择性的非甾体类糖皮质激素受体 (GR) 拮抗剂,Ki 为 210 nM。

规格 价格 是否有货 数量
2mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.

IC50&Target

Ki: 210 nM (GR)

体外研究

AL 082D06 (D06) binds specifically to GR with nanomolar affinity. Addition of AL 082D06 causes a dose-dependent decrease in transcriptional activation from the MMTV:Luc reporter stimulated with half-maximal DEX concentrations. AL 082D06 acts to antagonize reporter activity using several glucocorticoid-responsive promoter- reporter systems including the 3-kb tyrosine amino transferase (TAT) promoter and less complex promoters comprised of isolated glucocorticoid response element (GRE) sequences. AL 082D06 competes with H-Dex for baculovirus-expressed GR with nanomolar affinity. Other intracellular receptors (AR, ER, PR, and MR) have no affinity for AL 082D06 in a similarly structured binding assay with the appropriate receptor and tritiated ligand (>2500 nM). AL 082D06 has no activation efficacy on the progesterone, androgen, mineralocorticoid, retinoid, glucocorticoid, or estrogen receptors. AL 082D06 is very efficacious at antagonizing GR activity but exhibits much weaker efficacy when tested against the other steroid receptors in contrast to the reference antagonists used as controls.

分子式
C23H24N3O2Cl
分子量
409.91
CAS号
256925-03-8
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 : 7.5 mg/mL (18.30 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4396 mL 12.1978 mL 24.3956 mL
5 mM 0.4879 mL 2.4396 mL 4.8791 mL
10 mM 0.2440 mL 1.2198 mL 2.4396 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。

科研文献
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动物实验计算换算器
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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,

体内配方配制方法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

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。