AGN 192403 hydrochloride
目录号 : GC14934I1 imidazoline receptor
Cas No.:1021868-90-5
Sample solution is provided at 25 µL, 10mM.
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AGN 192403 hydrochloride is a selective ligand of imidazoline1 receptor [1].
Imidazoline receptor is the primary receptor for clonidine and other imidazolines. Imidazoline1 receptor (I1 receptor) lowers blood pressure via inhibition of the sympatho actions by imidazolines.
AGN 192403 hydrochloride is a selective ligand of I1 receptor. AGN192403 exhibited affinity for I1 receptor with Ki value of 42 nM and was only 5-fold less potent than clonidine. However, AGN192403 had no agonist and antagonist activities. In monkey and rat, AGN192403 (5000 μg/kg) had no effect on blood pressure [1]. In astrocytes, AGN 192403 inhibited cytochrome c release, lysosomal acridine orange relocation, caspase-9 activation and decrease in mitochondrial potential, cytotoxicities that was induced by naphthazarin. Also, AGN 192403 inhibited mitochondrial dysfunction and cytotoxicities induced by antimycin A and rotenone, inhibitors of mitochondrial respiration [2]. In isolated normotensive rat hearts, AGN192403 inhibited atrial natriuretic peptide (ANP) release induced by moxonidine (10−6 M) [3].
References:
[1] unk SA1, Lai RK, Burke JE,Munk SA1, Lai RK, Burke JE,Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent.Munk et al (1996) Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J.Med.Chem. 39 1193. PMID: 8632424.Stephen A. Munk,* Ronald K. Lai, James E. Burke, [1]. Munk SA, Lai RK, Burke JE, et al. Synthesis and Pharmacologic Evaluation of 2-endo-Amino-3-exoisopropylbicyclo[2.2.1]heptane: A Potent Imidazoline1 Receptor Specific Agent. J Med Chem, 1996, 39(6): 1193-1195.
[2]. Choi DH, Kim DH, Park YG, et al. Protective effects of rilmenidine and AGN 192403 on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. Free Radic Biol Med, 2002, 33(10): 1321-1333.
[3]. Mukaddam-Daher S, Menaouar A, Gutkowska J. Receptors involved in moxonidine-stimulated atrial natriuretic peptide release from isolated normotensive rat hearts. Eur J Pharmacol, 2006, 541(1-2): 73-79.
| Cas No. | 1021868-90-5 | SDF | |
| 化学名 | (1R,2R,3R,4S)-3-isopropylbicyclo[2.2.1]heptan-2-amine hydrochloride | ||
| Canonical SMILES | CC([C@]1([H])[C@@]2([H])CC[C@]([C@@]1([H])N)([H])C2)C.Cl | ||
| 分子式 | C10H19N.HCl | 分子量 | 189.73 |
| 溶解度 | Soluble to 100 mM in Water | 储存条件 | Store at RT |
| 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 | 5.2706 mL | 26.3532 mL | 52.7065 mL |
| 5 mM | 1.0541 mL | 5.2706 mL | 10.5413 mL |
| 10 mM | 0.5271 mL | 2.6353 mL | 5.2706 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