| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
AGN 192836 targets alpha2-adrenergic receptors, specifically the alpha2A, alpha2B, and alpha2C subtypes. It exhibits sub-nanomolar binding affinity with Ki values of 1.7 nM for alpha2A, 82 nM for alpha2B, and 19 nM for alpha2C. Functional EC50 values are 8.7 nM for alpha2A, 41 nM for alpha2B, and 6.6 nM for alpha2C.
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| ln Vitro |
According to binding assays, AGN 192836 exhibits a selectivity for α2A receptors that is 1200 times greater than that of α1 receptors, 50 times greater than that of α2B receptors, and 10 times greater than that of α2A receptors. ..α2C receptor [1].
AGN 192836 demonstrates potent in vitro activity as a selective alpha2-adrenergic agonist. It shows potent functional activity with EC50 values of 8.7 nM for alpha2A, 41 nM for alpha2B, and 6.6 nM for alpha2C receptors. The compound exhibits sub-nanomolar binding affinity (Ki 1.7 nM for alpha2A). |
| ln Vivo |
AGN 192836 proved to be more successful than brimonidine in lowering blood pressure when given intravenously in monkeys and as effective as brimonidine in lowering intraocular pressure when applied topically in rabbits [1].
In vivo, AGN 192836 modulates neurotransmitter release and physiological responses such as blood pressure and intraocular pressure by activating alpha2A/alpha2B/alpha2C adrenergic receptors. As a selective alpha2-adrenergic agonist, it is used in research to study adrenergic receptor signaling and related physiological functions. |
| Enzyme Assay |
In vitro receptor binding assays for AGN 192836 typically employ membrane preparations from cells expressing recombinant human alpha2A, alpha2B, or alpha2C adrenergic receptors. Radioligand binding assays using [3H]-RX821002 or other appropriate radioligands are performed to determine binding affinity (Ki). Competition binding experiments are conducted with varying concentrations of the compound.
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| Cell Assay |
In vitro cellular assays for AGN 192836 involve treating cells expressing alpha2-adrenergic receptors with varying concentrations of the compound (typically 0.001-100 microM range). Readouts include measurement of downstream signaling pathway activation (e.g., inhibition of adenylyl cyclase, decreased cAMP levels), assessment of receptor internalization, and functional assays such as [3⁵S]GTPgammaS binding to measure receptor activation.
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| Animal Protocol |
In vivo animal studies for AGN 192836 typically involve administration in rodent models to assess effects on blood pressure, intraocular pressure, and other alpha2-adrenergic receptor-mediated physiological responses. Dose-response studies determine the compound's efficacy and potency in vivo. The compound is used as a research tool to study alpha2-adrenergic receptor pharmacology.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of AGN 192836 are characteristic of small molecule alpha2-adrenergic agonists. With a molecular weight of 231.25, the compound is likely to have favorable oral bioavailability. PK parameters including half-life, Cmax, Tmax, and AUC would be determined via LC-MS/MS analysis following administration in appropriate animal models.
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| Toxicity/Toxicokinetics |
AGN 192836 is a research-grade compound for laboratory use only. As with all research chemicals, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. Comprehensive toxicology data including acute toxicity and repeat-dose toxicity studies are not publicly available.
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| References |
[1]. Stephen M, et al. Synthesis and Evaluation of 2-(Arylamino)imidazoles as α2-Adrenergic Agonists. J. Med. Chem., 1997, 40 (1), pp 18–23
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| Additional Infomation |
AGN 192836 (CAS# 171102-29-7) is a potent and selective alpha2-adrenergic receptor agonist used as a research tool. It is not approved for clinical use. The compound is typically stored at -20degC under desiccated conditions. It is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C12H13N3O2
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|---|---|
| Molecular Weight |
231.250522375107
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| Exact Mass |
231.1
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| CAS # |
171102-29-7
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| PubChem CID |
10176999
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
264
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC2=C1OCCO2)NC3=NC=CN3
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| InChi Key |
NDFYRGCPDAFQDG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H13N3O2/c1-8-9(15-12-13-4-5-14-12)2-3-10-11(8)17-7-6-16-10/h2-5H,6-7H2,1H3,(H2,13,14,15)
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| Chemical Name |
N-(5-methyl-2,3-dihydro-1,4-benzodioxin-6-yl)-1H-imidazol-2-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~80 mg/mL (~345.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3243 mL | 21.6216 mL | 43.2432 mL | |
| 5 mM | 0.8649 mL | 4.3243 mL | 8.6486 mL | |
| 10 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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