| Size | Price | Stock | Qty |
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| 10mg |
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| 100mg |
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| Targets |
Org-12962 targets serotonin (5-HT) receptors, specifically the 5-HT2C, 5-HT2A, and 5-HT2B receptor subtypes. It is a potent agonist at the 5-HT2C receptor with a pEC50 of 7.01. It also exhibits high efficacy at the 5-HT2A and 5-HT2B receptors with pEC50 values of 6.38 and 6.28, respectively. The 5-HT2C receptor is a G protein-coupled receptor that is widely expressed in the central nervous system and is involved in the regulation of mood, anxiety, appetite, and motor behavior. By activating 5-HT2C receptors, Org-12962 modulates neurotransmission in brain regions implicated in these processes. The compound's activity at other 5-HT2 receptor subtypes may contribute to its overall pharmacological profile.
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| ln Vitro |
In vitro studies have characterized Org-12962 as a potent agonist at the 5-HT2C receptor. Its activity is typically measured using functional assays, such as calcium mobilization or inositol phosphate accumulation, in cells expressing the human 5-HT2C receptor. The pEC50 for 5-HT2C receptor activation is 7.01. Org-12962 also shows high efficacy at the 5-HT2A and 5-HT2B receptors with pEC50 values of 6.38 and 6.28, respectively. These in vitro studies confirm that Org-12962 is a potent agonist at multiple 5-HT2 receptor subtypes. Its selectivity for the 5-HT2C receptor over other serotonin receptor subtypes has been characterized, but specific data is not detailed in the available literature.
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| ln Vivo |
After injection, the frequency threshold for self-interruption was markedly elevated by Org-12962 (ip; 0.3-3.2 mg/kg) (F3.71=11.40). 0.3% v/v Tween 80 is added to physiological saline (NaCl0.9%), which is used to dissolve or gently suspend Org-12962 [1].
In vivo studies have demonstrated that Org-12962 exhibits antiaversive effects in animal models of anxiety. In a rat model of panic-like anxiety, intraperitoneal injection of Org-12962 at doses of 0.3-3.2 mg/kg significantly increases the postinjection frequency thresholds for self-interruption, indicating an antiaversive effect. The compound is dissolved or microsuspended in 0.3% v/v Tween 80 in physiological saline for administration. These findings suggest that 5-HT2C receptor agonism may have potential in the treatment of anxiety disorders. Org-12962 is used as a research tool to study the role of 5-HT2C receptors in anxiety and other behavioral processes. |
| Enzyme Assay |
The in vitro receptor binding and functional assays for Org-12962 are designed to characterize its activity at serotonin receptors. Receptor binding assays would typically involve competition binding studies using radiolabeled ligands specific for 5-HT2A, 5-HT2B, and 5-HT2C receptors expressed in cell membranes. Functional assays measure the compound's ability to activate these receptors. For 5-HT2C receptor agonism, the most common assay is the measurement of calcium mobilization or inositol phosphate accumulation in cells expressing the human 5-HT2C receptor. Cells are loaded with a calcium-sensitive dye or pre-labeled with [3H]-myo-inositol, and the response to Org-12962 is measured. The pEC50 for 5-HT2C receptor activation is 7.01. Similar assays are performed for 5-HT2A and 5-HT2B receptors to determine the pEC50 values of 6.38 and 6.28, respectively. These assays provide a comprehensive pharmacological profile of Org-12962.
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| Cell Assay |
In vitro cell-based assays for Org-12962 are used to study its effects on serotonin receptor signaling. Cells expressing human 5-HT2A, 5-HT2B, or 5-HT2C receptors (e.g., CHO-K1 cells) are treated with Org-12962, and downstream signaling is measured. For Gq-coupled 5-HT2 receptors, the most common readout is the measurement of intracellular calcium mobilization using a fluorescent calcium indicator. The pEC50 for each receptor subtype is determined from dose-response curves. These cell-based assays confirm that Org-12962 is a potent agonist at these receptors and provide data on its efficacy and potency in a cellular context.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat [2]
Doses: 0.3 mg/kg, 1 mg/kg, 3.2 mg/kg Route of Administration: intraperitoneal (ip) injection; 0.3-3.2 mg/kg Experimental Results: Induced dose-related anti-panic-like effects. In vivo animal experiments for Org-12962 have been conducted in rat models of anxiety. In a typical study, rats are administered Org-12962 by intraperitoneal injection at doses ranging from 0.3 to 3.2 mg/kg. The compound is dissolved or microsuspended in 0.3% v/v Tween 80 in physiological saline. The antiaversive effects of Org-12962 are assessed using a model of panic-like anxiety, such as the elevated plus maze or the shock-probe burying test. In one study, Org-12962 significantly increased the postinjection frequency thresholds for self-interruption, indicating an antiaversive effect. These experiments demonstrate the in vivo efficacy of Org-12962 and support the role of 5-HT2C receptors in anxiety modulation. |
| ADME/Pharmacokinetics |
Org-12962 has a molecular weight of 265.66 g/mol and a molecular formula of C10H11ClF3N3. It is a solid compound. For research use, Org-12962 is typically supplied as a powder. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month. The compound is stable under recommended storage conditions. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied, and Org-12962 is reported to be orally active.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Org-12962 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vivo studies have used doses up to 3.2 mg/kg in rats without reported overt toxicity. However, comprehensive toxicological studies, including acute and chronic toxicity studies, have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling Org-12962. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References |
[1]. Porter RH,et al. Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cells.Br J Pharmacol. 1999 Sep;128(1):13-20.
[2]. Jenck F, et al. Antiaversive effects of 5HT2C receptor agonists and fluoxetine in a model of panic-like anxiety in rats.Eur Neuropsychopharmacol. 1998 Aug;8(3):161-8. [3]. Faassen F, et al. Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.Int J Pharm. 2003 Sep 16;263(1-2):113-22. |
| Additional Infomation |
Org-12962 is a research compound and is not approved for any clinical or therapeutic use. It is a potent, selective, and orally active agonist of the 5-HT2C receptor with a pEC50 of 7.01. Org-12962 also exhibits high efficacy at the 5-HT2A and 5-HT2B receptors with pEC50 values of 6.38 and 6.28, respectively. Org-12962 displays antiaversive effects in a rat model of panic-like anxiety. It is used as a research tool to study the role of 5-HT2C receptors in anxiety, mood, and other behavioral processes. The compound's mechanism of action involves activating 5-HT2C receptors, which modulates neurotransmission in brain regions involved in these processes.
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| Molecular Formula |
C10H11CLF3N3
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| Molecular Weight |
265.6642
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| Exact Mass |
265.059
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| CAS # |
132834-56-1
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| Related CAS # |
Org-12962 hydrochloride;210821-63-9
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| PubChem CID |
9796408
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| Appearance |
White to light yellow solid powder
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| Density |
1.454g/cm3
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| Boiling Point |
286.004ºC at 760 mmHg
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| Flash Point |
126.771ºC
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| Vapour Pressure |
0.001mmHg at 25°C
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| Index of Refraction |
1.541
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| LogP |
2.557
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
256
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C(F)(F)F)C([H])=C([H])C(=N1)N1C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H]
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| InChi Key |
QZYYPQAYSFBKPW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11ClF3N3/c11-9-7(10(12,13)14)1-2-8(16-9)17-5-3-15-4-6-17/h1-2,15H,3-6H2
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| Chemical Name |
1-[6-chloro-5-(trifluoromethyl)pyridin-2-yl]piperazine
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| Synonyms |
Org-12962 Org12962 Org 12962
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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 : ~250 mg/mL (~941.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (8.17 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 21.7 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: ≥ 2.17 mg/mL (8.17 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 21.7 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. View More
Solubility in Formulation 3: ≥ 2.17 mg/mL (8.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7642 mL | 18.8210 mL | 37.6421 mL | |
| 5 mM | 0.7528 mL | 3.7642 mL | 7.5284 mL | |
| 10 mM | 0.3764 mL | 1.8821 mL | 3.7642 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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