| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
5-HT2B Receptor 9.8 (pKi) 5-HT2A Receptor 7.7 (pKi) 5-HT2C Receptor 7.6 (pKi)
LY266097 hydrochloride targets the serotonin 5-HT2B receptor with high selectivity. It is a selective antagonist with a pKi of 9.3 (or 9.8) for 5-HT2B. The compound shows more than 100-fold selectivity over 5-HT2A (pKi = 7.7) and 5-HT2C (pKi = 7.6) receptors. By blocking 5-HT2B receptors, the compound modulates serotonergic signaling pathways involved in mood, cardiovascular function, and neurotransmitter release. |
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| ln Vitro |
With a pKi of 9.7 for the human cloned 5-HT2B receptor and 100-fold higher selectivity over the human 5-HT2C and 5-HT2A sites, LY266097 is an extremely selective 5-HT2B receptor antagonist[2].
In vitro, LY266097 hydrochloride acts as a selective 5-HT2B receptor antagonist. Its activity is typically assessed by measuring its ability to inhibit agonist-induced calcium mobilization or inositol phosphate accumulation in cells expressing 5-HT2B receptors. The compound shows pKi values of 7.7, 9.8, and 7.6 for human 5-HT2A, 5-HT2B, and 5-HT2C, respectively. Standard in vitro assays include receptor binding studies using radiolabeled ligands and functional assays measuring calcium signaling or phosphoinositide hydrolysis. |
| ln Vivo |
The 2-day injection of 0.6 mg/kg of LY266097 reverses the reduction in dopamine (DA) caused by escitalopram[1]. Pyramidal neuron firing and burst activity are increased when LY266097 is administered either on its own or in conjunction with escapilopram over the final three days of a 14-day regimen[1].
In vivo, LY266097 hydrochloride attenuates amphetamine-induced locomotor activity in rats. As a selective 5-HT2B receptor antagonist, it would be expected to modulate serotonergic signaling and affect behaviors related to mood and motor function. The compound can be used in studies about depression. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool to study 5-HT2B receptor function. |
| Enzyme Assay |
For non-cell-based receptor binding assays, LY266097 hydrochloride can be evaluated using membrane preparations from cells expressing human 5-HT2A, 5-HT2B, or 5-HT2C receptors. Radioligand binding displacement experiments are performed using suitable radiolabeled ligands such as [3H]-ketanserin for 5-HT2A, [3H]-mesulergine for 5-HT2C, or [3H]-5-HT for 5-HT2B. 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 ligand. pKi values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human 5-HT2B 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 pre-incubated with various concentrations of LY266097 hydrochloride. Receptor activation is stimulated by the addition of a 5-HT2B receptor agonist such as 5-HT or BW723C86. Fluorescence intensity is measured using a fluorescence plate reader. The reduction in calcium signal compared to control wells indicates antagonist activity. IC50 or pA2 values are calculated from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats weighing 250-350 g[1]
Doses: 0.6 mg/kg Route of Administration: Administered ip alone or concomitantly with Escitalopram (2 mg/kg) for 2 days Experimental Results: Short -term administration (0.6 mg/kg/day for 2 days; ip) alone had no effect on these parameters, its co-administration counteracted the inhibitory effect of escitalopram on the firing activity of DA neurons, resulting in a recovery to control level. For in vivo animal studies, LY266097 hydrochloride can be administered to rodents via intraperitoneal injection. In models of amphetamine-induced hyperactivity, locomotor activity is measured following compound administration. In models of depression, behavioral tests such as the forced swim test or tail suspension test may be performed. Dosing regimens vary depending on the specific model and desired exposure levels. Blood and tissue samples may be collected for pharmacokinetic analysis. |
| ADME/Pharmacokinetics |
LY266097 hydrochloride has a molecular weight of 407.33 and a molecular formula of C21H23ClN2O2·HCl. It is a selective 5-HT2B receptor antagonist with a pKi of 9.8 for 5-HT2B. The compound is supplied as a research-grade compound. It is soluble in DMSO. It should be stored at -20°C for long-term stability. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of LY266097 hydrochloride has not been extensively reported. As a 5-HT2B receptor antagonist, potential adverse effects may include modulation of serotonergic signaling, which could affect mood, cardiovascular function, and gastrointestinal motility. 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.
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| References | |
| Additional Infomation |
LY266097 hydrochloride (CAS 172895-39-5) is a selective 5-HT2B receptor antagonist. It exhibits pKi values of 7.7, 9.8, and 7.6 for human 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. It shows more than 100-fold selectivity for 5-HT2B over 5-HT2A and 5-HT2C. LY266097 hydrochloride attenuates amphetamine-induced locomotor activity in rats and can be used in studies about depression. It is available for research purposes only.
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| Molecular Formula |
C21H24CL2N2O2
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|---|---|
| Molecular Weight |
407.33
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| Exact Mass |
406.121
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| CAS # |
172895-39-5
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| PubChem CID |
9953184
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
5.707
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1)NC3=C2CCNC3CC4=C(C(=C(C=C4)OC)OC)Cl.Cl
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| InChi Key |
KPXKZZURYAXZQE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23ClN2O2.ClH/c1-12-4-6-16-15(10-12)14-8-9-23-17(20(14)24-16)11-13-5-7-18(25-2)21(26-3)19(13)22;/h4-7,10,17,23-24H,8-9,11H2,1-3H3;1H
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| Chemical Name |
1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;hydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (153.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.11 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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 | 2.4550 mL | 12.2751 mL | 24.5501 mL | |
| 5 mM | 0.4910 mL | 2.4550 mL | 4.9100 mL | |
| 10 mM | 0.2455 mL | 1.2275 mL | 2.4550 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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