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RU 24969 hemisuccinate 66611-27-6

RU 24969 hemisuccinate 66611-27-6

CAS No.: 66611-27-6

RU 24969 hemisuccinate is a preferential 5-HT1B agonist/activator with a Ki of 0.38 nM. It also shows significant affini
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RU 24969 hemisuccinate is a preferential 5-HT1B agonist/activator with a Ki of 0.38 nM. It also shows significant affinity for the 5-HT1A receptor (Ki=2.5 nM) and has low affinity for other receptor sites in the brain. . RU 24969 hemisuccinate reduces fluid consumption and increases forward motion.

Physicochemical Properties


Molecular Formula C14H16N2O.1/2C4H6O4
Molecular Weight 287.34
Exact Mass 574.279
CAS # 66611-27-6
Related CAS # RU 24969;66611-26-5
PubChem CID 3050530
Appearance Typically exists as solid at room temperature
Hydrogen Bond Donor Count 6
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 7
Heavy Atom Count 42
Complexity 395
Defined Atom Stereocenter Count 0
SMILES

C(O)(=O)CCC(O)=O.COC1=CC=C2C(C(C3=CCNCC3)=CN2)=C1.COC1=CC=C2C(C(C3=CCNCC3)=CN2)=C1

InChi Key BNYJLRQAWCQJOM-UHFFFAOYSA-N
InChi Code

InChI=1S/2C14H16N2O.C4H6O4/c2*1-17-11-2-3-14-12(8-11)13(9-16-14)10-4-6-15-7-5-10;5-3(6)1-2-4(7)8/h2*2-4,8-9,15-16H,5-7H2,1H3;1-2H2,(H,5,6)(H,7,8)
Chemical Name

butanedioic acid;5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole
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

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets 5-HT1B Receptor 0.38 nM (Ki) 5-HT1A Receptor 2.5 nM (Ki)
ln Vitro In vitro, RU 24969 (10 μM) decreases the release of [3H]-5-HT from rat frontal cortex slices when activated by K+[2].
ln Vivo In water-deprived rats, RU 24969 (0.03-3.0 mg/kg; sc) reduces water consumption dose-dependently[1]. Forward locomotion is dose-dependently increased by RU 24969 (0.3–3.0 mg/kg; sc)[1].
Animal Protocol Animal/Disease Models: Male SD (Sprague-Dawley) rats[1]
Doses: 0.03, 0.3, 1.0, 3.0 mg/kg
Route of Administration: A single sc
Experimental Results: diminished water consumption Dramatically at dose of 0.3, 1.0, and 3.0 mg/kg.
References

[1]. RU 24969-produced adipsia and hyperlocomotion: differential role of 5HT 1A and 5HT 1B receptor mechanisms. Pharmacol Biochem Behav. 2014 Sep; 124: 1-4.

[2]. The 5-HT1 receptor agonist RU-24969 decreases 5-hydroxytryptamine (5-HT) release and metabolism in the rat frontal cortex in vitro and in vivo. Br J Pharmacol. 1985 Sep; 86(1): 209-16.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.4802 mL 17.4010 mL 34.8020 mL
5 mM 0.6960 mL 3.4802 mL 6.9604 mL
10 mM 0.3480 mL 1.7401 mL 3.4802 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.