| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
5-HT2B Receptor 9.8 (pKi) 5-HT2A Receptor 7.7 (pKi) 5-HT2C Receptor 7.6 (pKi)
|
|---|---|
| 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].
|
| 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].
|
| 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. |
| References |
| Molecular Formula |
C21H24CL2N2O2
|
|---|---|
| Molecular Weight |
407.33
|
| 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
|
| LogP |
5.707
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
27
|
| Complexity |
479
|
| Defined Atom Stereocenter Count |
0
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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
|
| Chemical Name |
1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 62.5 mg/mL (153.44 mM)
|
|---|---|
| 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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