| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
0.77 nM and 1.5 nM for rat and human 5-HT2 receptor[1]
AL-34662 targets the 5-HT2A receptor as a potent and selective agonist. It shows IC50 values of 0.77 nM for rat 5-HT2 receptors and 1.5 nM for human 5-HT2 receptors. The compound also exhibits weak α-1D adrenergic agonist activity with an EC50 of 0.4 μM. Its primary mechanism involves activation of 5-HT2A receptors, which mediates its ocular hypotensive effects. It also shows non-selective binding to other receptors. |
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| ln Vitro |
In vitro, AL-34662 demonstrates potent and selective 5-HT2A receptor agonist activity. It exhibits IC50 values of 0.77 nM for rat 5-HT2 receptors and 1.5 nM for human 5-HT2 receptors. The compound also shows weak α-1D adrenergic agonist activity with an EC50 of 0.4 μM. It is used in research to study 5-HT2A receptor function and its role in intraocular pressure regulation. The compound's selectivity for 5-HT2A over other receptors makes it a valuable pharmacological tool.
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| ln Vivo |
In vivo, AL-34662 is an ocular hypotensive agent used to lower intraocular pressure. It demonstrates efficacy in reducing intraocular pressure in cynomolgus monkeys. The compound's 5-HT2A receptor agonist activity mediates its ocular hypotensive effects. It has been studied for its potential in glaucoma research. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool for studying 5-HT2A receptor function and ocular pharmacology.
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| Enzyme Assay |
For non-cell-based receptor binding assays, AL-34662 can be evaluated using membrane preparations from cells expressing human or rat 5-HT2A receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-ketanserin. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at room temperature for 60-90 minutes. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ketanserin. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human or rat 5-HT2A receptors are cultured in appropriate media. For functional assays, intracellular calcium mobilization is measured using fluorescent calcium indicators such as Fluo-4 AM. Cells are loaded with the dye and treated with various concentrations of AL-34662. Fluorescence intensity is measured using a fluorescence plate reader. The increase in calcium signal compared to control wells indicates agonist activity. EC50 values are calculated from dose-response curves. For selectivity profiling, similar assays are performed using cells expressing other receptor subtypes.
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| Animal Protocol |
For in vivo animal studies, AL-34662 can be administered to rodents or non-human primates via topical ocular administration or injection. In models of ocular hypertension, intraocular pressure is measured using a tonometer following compound administration. In cynomolgus monkeys, the compound's ability to lower intraocular pressure is assessed. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
AL-34662 has a molecular weight of 191.23 and a molecular formula of C10H13N3O. It has a purity of >98% (HPLC) and is soluble in DMSO at 62.5 mg/mL (326.83 mM). The compound should be stored at -20°C and is stable for ≥2 years. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of AL-34662 has not been extensively reported. As a 5-HT2A receptor agonist, potential adverse effects may include modulation of serotonergic signaling, which could affect mood, perception, and cardiovascular function. The compound is for research use only and is not intended for human consumption. Standard toxicological evaluation would include acute and repeated-dose toxicity studies, as well as assessment of effects on the central nervous system and cardiovascular function.
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| References |
[1]. Sharif NA, et al. AL-34662: a potent, selective, and efficacious ocular hypotensive serotonin-2 receptor agonist. J Ocul Pharmacol Ther. 2007 Feb;23(1):1-13.
[2]. Asano T, et al. Ameliorative effect of chlorpromazine hydrochloride on visceral hypersensitivity in rats: possible involvement of 5-HT2A receptor. Br J Pharmacol. 2017 Oct;174(19):3370-3381. |
| Additional Infomation |
AL-34662 (CAS 210580-75-9) is a selective and potent 5-HT2A receptor agonist with IC50 values of 0.77 nM and 1.5 nM for rat and human 5-HT2 receptors, respectively. It is also a weak α-1D adrenergic agonist with an EC50 of 0.4 μM. AL-34662 is an ocular hypotensive agent used to lower intraocular pressure. It has been studied for its potential in glaucoma research. It is available for research purposes only.
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| Molecular Formula |
C10H13N3O
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|---|---|
| Molecular Weight |
191.23
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| Exact Mass |
191.105
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| CAS # |
210580-75-9
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| PubChem CID |
135453290
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
372.8±22.0 °C at 760 mmHg
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| Flash Point |
179.2±22.3 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.652
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| LogP |
0.81
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
200
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(CN1N=CC2=CC=C(C=C12)O)N
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| InChi Key |
WBYHTZYHAFNBKW-ZETCQYMHSA-N
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| InChi Code |
InChI=1S/C10H13N3O/c1-7(11)6-13-10-4-9(14)3-2-8(10)5-12-13/h2-5,7,14H,6,11H2,1H3/t7-/m0/s1
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| Chemical Name |
1-[(2S)-2-aminopropyl]indazol-6-ol
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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: 62.5 mg/mL (326.83 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2293 mL | 26.1465 mL | 52.2931 mL | |
| 5 mM | 1.0459 mL | 5.2293 mL | 10.4586 mL | |
| 10 mM | 0.5229 mL | 2.6147 mL | 5.2293 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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