SQ 22536
(Synonyms: 9-(四氢-2-呋喃)腺膘呤) 目录号 : GC13867An adenylyl cyclase inhibitor
Cas No.:17318-31-9
Sample solution is provided at 25 µL, 10mM.
SQ22536 is an effective adenylate cyclase (AC) inhibitor.
SQ22536 (SQ22,536) effectively inhibits the effect of forskolin with respective IC50 values of 5 μM.Preincubation with graded concentrations of SQ22536 reveals that both SQ22536 effectively inhibits PACAP-induced reporter gene activation with approximate IC50 value of 5 μM. SQ22536 more potently inhibits forskolin-induced Elk activation (IC50=10 μM) than 8-Br-cAMP-induced Elk activation (IC50=170 μM). Most notably, there are substantial differences in the reported potencies of SQ22536 to inhibit the activities of recombinant AC5 and AC6, with respective IC50 values of 2 μM and 360 μM. At a greater concentration (500 μM), SQ22536 significantly inhibits neurite elongation due to either forskolin or 8-Br-cAMP[1].
Reference:
[1]. Emery AC, et al. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536. Mol Pharmacol. 2013 Jan;83(1):95-105.
Cell experiment: |
HEK293 CRE-luc2P GloResponse luciferase reporter cells are transduced with retroviral vectors expressing rat PAC1hop receptors. Individual cell lines are obtained by limiting dilution cloning, and a clonal PAC1-expressing line is propagated and used for CRE luciferase assays. In brief, HEK293 CRE-luc2P cells are plated in 96-well plates (10,000 cells in 80 μL media per well) in assay media (DMEM supplemented with 1% fetal bovine serum). One day after plating, cells are treated with AC inhibitors (10 μL in assay media/well) for 30 minutes, followed by agonists (10 μL in assay media/well), and are incubated for 4 hours. Luciferase activity is determined after the addition of 100 μL/well Bright-Glo Luciferase Assay Reagent. Luminescence (RLU) is measured in a Victor3 microtiter plate reader after 2 minutes of agitation at room temperature. Cyclic AMP is measured in NS-1 cells. In brief, NS-1 cells are seeded and grown overnight in 96-well plates. The next day, cells are pretreated for 20 minutes in media containing the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (0.5 mM) with or without SQ22536. After pretreatment with inhibitors, cells are stimulated with agonists, added as 10× solutions, for an additional 20 minutes. Intracellular cAMP is then assayed using the cAMP Biotrak enzyme immunoassay kit for measurement of nonacetylated cAMP[1]. |
References: [1]. Emery AC, et al. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536. Mol Pharmacol. 2013 Jan;83(1):95-105. |
Cas No. | 17318-31-9 | SDF | |
别名 | 9-(四氢-2-呋喃)腺膘呤 | ||
化学名 | (R)-9-(tetrahydrofuran-2-yl)-9H-purin-6-amine | ||
Canonical SMILES | NC(N=CN=C12)=C2N=CN1[C@@H]3OCCC3 | ||
分子式 | C9H11N5O | 分子量 | 205.22 |
溶解度 | ≥ 20.5mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 4.8728 mL | 24.3641 mL | 48.7282 mL |
5 mM | 0.9746 mL | 4.8728 mL | 9.7456 mL |
10 mM | 0.4873 mL | 2.4364 mL | 4.8728 mL |
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 | g | 每只动物给药体积 | ul | 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GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
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,
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 saline,混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet