| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
RU-24,969 targets the 5-HT1A and 5-HT1B serotonin receptors, which are G protein-coupled receptors involved in the regulation of mood, anxiety, and addiction. It acts as a potent and selective agonist at these receptors, with a Ki of 0.38 nM for 5-HT1B and 2.5 nM for 5-HT1A. By activating 5-HT1B receptors, RU-24,969 modulates neurotransmitter release and neuronal activity, affecting various physiological and behavioral processes. The compound has low affinity for other receptor sites in the brain.
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| ln Vitro |
In vitro, RU 24969 (10 μM) decreases K+-stimulated [3H]-5-HT release in rat frontal brain slices [2].
In vitro, RU-24,969 acts as a potent and selective agonist at 5-HT1A and 5-HT1B receptors, with Ki values of 2.5 nM and 0.38 nM, respectively. It preferentially activates 5-HT1B receptors. In rat frontal brain slices, RU 24969 (10 μM) decreases K+-stimulated [3H]-5-HT release. The compound's ability to activate 5-HT1B receptors has been confirmed in various cell-based assays measuring receptor-mediated signaling, such as inhibition of cAMP accumulation. |
| ln Vivo |
In dehydrated rats, RU 24969 (0.03–3.0 mg/kg; subcutaneous injection) decreases water consumption in a dose-dependent manner [1]. Subcutaneous injection of RU 24969 (0.3–3.0 mg/kg) enhances forward motility in a dose-dependent manner [1].
In vivo, RU-24,969 has been shown to affect behavior in animal models. In dehydrated rats, RU 24969 (0.03–3.0 mg/kg; subcutaneous injection) decreases water consumption in a dose-dependent manner. Subcutaneous injection of RU 24969 (0.3–3.0 mg/kg) enhances forward motility in a dose-dependent manner. RU-24,969 has been found to increase the reinforcing properties of cocaine, suggesting a role for 5-HT1B receptors in cocaine addiction. The compound is used to study the role of 5-HT1B receptors in addiction and other behavioral disorders. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for RU-24,969 are radioligand binding assays using membrane preparations from cells expressing recombinant 5-HT1A or 5-HT1B receptors. The compound's binding affinity (Ki) is determined by its ability to displace a labeled serotonin receptor ligand such as [3H]8-OH-DPAT or [3H]GR125743. Functional assays such as [35S]GTPγS binding or cAMP accumulation assays are used to measure the compound's agonist activity at these receptors.
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| Cell Assay |
In vitro cellular assays for RU-24,969 are performed using cell lines expressing 5-HT1A or 5-HT1B receptors, such as CHO or HEK293 cells. Cells are treated with varying concentrations of RU-24,969, and receptor activation is assessed by measuring the inhibition of forskolin-stimulated cAMP accumulation (since 5-HT1 receptors are Gi-coupled). The EC50 for inhibition of cAMP accumulation is determined from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat[1]
Doses: 0.03, 0.3, 1.0, 3.0 mg/kg Route of Administration: Single subcutaneous injection Experimental Results: Water consumption was Dramatically diminished at doses of 0.3, 1.0 and 3.0 mg/kg . In vivo animal experiments for RU-24,969 are conducted in rodent models. In dehydrated rats, RU 24969 is administered subcutaneously at doses of 0.03–3.0 mg/kg, and water consumption is measured. In locomotor activity studies, rats are injected subcutaneously with RU 24969 (0.3–3.0 mg/kg), and forward motility is assessed. Cocaine self-administration studies are used to evaluate the compound's effects on reinforcing properties. |
| ADME/Pharmacokinetics |
RU-24,969 has a molecular weight of 228.3 g/mol and a molecular formula of C14H16N2O. It is a light yellow to yellow solid powder with a logP of 2.882. The compound should be stored under recommended conditions. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a research compound, RU-24,969 is primarily used in in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
The toxicological profile of RU-24,969 has not been extensively characterized. As a serotonin receptor agonist, the compound may have potential effects on mood, behavior, and cardiovascular function. No significant toxicity has been reported in the available literature. Standard toxicology studies would be necessary to establish its safety profile. The compound is a research tool and is not intended for human use.
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| References |
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| Additional Infomation |
5-Methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole is a member of the indole class of compounds.
RU-24,969 is a potent and selective agonist of the 5-HT1A and 5-HT1B serotonin receptors. It is also known as RU 24969. RU-24,969 preferentially activates 5-HT1B receptors with a Ki of 0.38 nM. The compound is used to study the role of 5-HT1B receptors in cocaine addiction and other behavioral disorders. RU-24,969 is a research compound and is not an approved drug. |
| Molecular Formula |
C14H16N2OM
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| Molecular Weight |
228.3
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| Exact Mass |
228.126
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| Elemental Analysis |
C, 73.66; H, 7.06; N, 12.27; O, 7.01
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| CAS # |
66611-26-5
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| Related CAS # |
RU 24969 succinate;107008-28-6;RU 24969 hemisuccinate;66611-27-6
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| PubChem CID |
108029
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.882
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
303
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KRVMLPUDAOWOGN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N2O/c1-17-11-2-3-14-12(8-11)13(9-16-14)10-4-6-15-7-5-10/h2-4,8-9,15-16H,5-7H2,1H3
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| Chemical Name |
5-Methoxy-3-(1,2,5,6-tetrahydro-4-pyridinyl)-1H-indole hemisuccinate
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| Synonyms |
RU 24,969 RU-24,969 RU24,969RU 24969 RU-24969 RU24969
RU 24969 hemisuccinate RU 24969 RU-24969 RU24969.
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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 : ≥ 30 mg/mL (~131.41 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.95 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 (10.95 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 | 4.3802 mL | 21.9010 mL | 43.8020 mL | |
| 5 mM | 0.8760 mL | 4.3802 mL | 8.7604 mL | |
| 10 mM | 0.4380 mL | 2.1901 mL | 4.3802 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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