| 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 |
| Targets |
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| ln Vitro |
For cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, and 5-HT7 receptors, SB 243213 hydrochloride exhibits little affinity (pKi<6). It has moderate affinity for the cloned human D2 receptor (pKi=6.7) and weak affinity for the cloned human 5-HT1D and D3 receptors (pKi<6.5) [1]. SB 243213 hydrochloride has 100-fold selectivity for a range of enzymes, ion channels, and neurotransmitter receptors [1].
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| ln Vivo |
Rats' duration of social interaction during a 15-minute period in a brightly lighted, unfamiliar test box is increased dose-dependently and considerably by SB 243213 hydrochloride (0.1–10 mg/kg, po 1 h pre-test)[1]. One hour before the exam, 0.3 mg/kg of SB 243213 hydrochloride po improves social contact time significantly[1].
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| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) experimentally naive rats (220-300 g)[1]
Doses: 0.1 , 0.3, 1, 3, 10 mg/kg Route of Administration: PO; 1 hour pre-test Experimental Results: Dose-dependently and Dramatically increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box . |
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| References |
[1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99.
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| Molecular Formula |
C22H21CL2F3N4O2
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|---|---|
| Molecular Weight |
501.33
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| Exact Mass |
500.099
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| CAS # |
200940-23-4
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| Related CAS # |
SB 243213;200940-22-3;SB 243213 dihydrochloride;1780372-25-9
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| PubChem CID |
15981450
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.577
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
634
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(F)(F)F)C=C2C(CCN2C(NC2=CC=C(OC3=CC=CN=C3C)N=C2)=O)=C1
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| InChi Key |
OOOGUILTDUSZPA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19F3N4O2.ClH/c1-13-10-15-7-9-29(18(15)11-17(13)22(23,24)25)21(30)28-16-5-6-20(27-12-16)31-19-4-3-8-26-14(19)2;/h3-6,8,10-12H,7,9H2,1-2H3,(H,28,30);1H
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| Chemical Name |
5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide;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, avoid exposure to moisture. |
| 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: ~20 mg/mL (~43.0 mM; with ultrasonication and warming by heating to 60°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (20.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 mg/mL (4.30 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 DMSO stock solution (20.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 2 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (20.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9947 mL | 9.9735 mL | 19.9469 mL | |
| 5 mM | 0.3989 mL | 1.9947 mL | 3.9894 mL | |
| 10 mM | 0.1995 mL | 0.9973 mL | 1.9947 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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