AGN 192403 hydrochloride |
| Catalog No.GC14934 |
I1 imidazoline receptor
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | (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 | ||
| Formula | C10H19N.HCl | M.Wt | 189.73 |
| Solubility | Soluble to 100 mM in Water | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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