SR59230A
目录号 : GC39725
A β3-AR antagonist
Cas No.:174689-39-5
Sample solution is provided at 25 µL, 10mM.
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SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).1 It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).2 At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.3 In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway.4 It has also been used in studies of heart failure to elucidate the role of the β3-ARs.5
1.Manara, L., Badone, D., Baroni, M., et al.Functional identification of rat atypical β-adrenoceptors by the first β3-selective antagonists, aryloxypropanolaminotetralinsBr. J. Pharmacol.117(3)435-442(1996) 2.Hoffman, C., Leitz, M.R., Oberdorf-Maass, S., et al.Comparative pharmacology of human β-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cellsNaunyn-Schmiedeberg's Arch. Pharmacol.369(2)151-159(2004) 3.Bexis, S., and Docherty, J.R.Role of α1- and β3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouseBr. J. Pharmacol.158(1)259-266(2009) 4.Mizuno, K., Kanda, Y., Kuroki, Y., et al.Stimulation of β3-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytesBr. J. Pharmacol.135(4)951-960(2002) 5.Gan, R.T., Li, W.M., Xiu, C.H., et al.Chronic blocking of β3-adrenoceptor ameliorates cardiac function in rat model of heart failureChin. Med. J. (Engl.)120(24)2250-2255(2007)
| Cas No. | 174689-39-5 | SDF | |
| Canonical SMILES | O[C@@H](CN[C@H]1CCCC2=C1C=CC=C2)COC3=CC=CC=C3CC.O=C(O)C(O)=O | ||
| 分子式 | C23H29NO6 | 分子量 | 415.48 |
| 溶解度 | DMSO: 31.25 mg/mL (75.21 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4069 mL | 12.0343 mL | 24.0685 mL |
| 5 mM | 0.4814 mL | 2.4069 mL | 4.8137 mL |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4069 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