| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
SB-242084 HCl, the hydrochloride salt of SB 242084, is a novel, potent and selective 5-HT2C receptor antagonist with pKi of 9.0 and with 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. Anxiolytic effects are exhibited by the psychoactive compound SB-242084. It can enhance dopamine signaling in the limbic system, as well as having complex effects on the dopamine release produced by cocaine, increasing it in some brain regions but reducing it in others. It has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants, and may also reduce their side effects. In experiments on animals, SB-242084 exhibited stimulant-type activity and reinforcing effects that were comparatively milder than those of cocaine or amphetamines.
| ln Vitro |
SB 242084 dihydrochloride (100 nM; 45 min) exhibits antagonism of the 5-HT-stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT2C receptor in SH-SY5Y cells [1]. SB 242084 dihydrochloride (1-100 nM; 24 hours) increases RPTC respiration and PGC-1α mRNA expression [2]. Cell Viability Assay [1] Cell Line: SH-SY5Y Cell Concentration: 100 nM Incubation Time: 45 minutes Results: Antagonizes the concentration-related increase in PI hydrolysis induced by 5-HT. RT-PCR[2] Cell Line: RPTC Cell Concentration: 1-100 nM Incubation Time: 24 hours Results: FCCP uncouples respiration and increases PGC-1α mRNA expression.
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| ln Vivo |
SB 242084 dihydrochloride (0.1-1 mg/kg; i.p.; single dose; 20 minutes before testing) improves rat behavior in social interaction tests [1]. SB 242084 dihydrochloride (5 mg/kg; intraperitoneal injection; single dose; 20 minutes before testing) improves mCPP-induced hypophagia in rats [1]. SB 242084 diHClide (5, 10 mg/kg; i.p.; single dose) increases basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) levels in the nucleus accumbens of rats [3]. SB 242084 Dihydrochloride (160-640 µg/kg; IV; single dose) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons and bursting in the same region in vivo Activity is also enhanced. 3]. Animal model: Male Sprague-Dawley (CD) rat [1]. Dose: 0.1-1 mg/kg Administration: Intraperitoneal injection; singleton; 20 minutes Pre-test results: Rats spent more than 15 minutes in social interaction under bright light conditions and in unfamiliar test box ,A significant increase. Animal model: Male Sprague-Dawley (CD) rat (mCPP-induced hypophagia model) [1]. Dose: 5 mg/kg Administration: Intraperitoneal injection; singleton; 20 min Pre-test results: 23-h food-deprived rats consumed significantly less food during the 1-h test period from the date of food presentation. Animal model: rat[2]. Dosage: 5, 10 mg/kg Administration: intraperitoneal injection; Single result: Significant increase in basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.
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| References |
| Molecular Formula |
C21H21CL3N4O2
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|---|---|
| Molecular Weight |
467.7760
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| Exact Mass |
466.07
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| Elemental Analysis |
C, 53.92; H, 4.53; Cl, 22.74; N, 11.98; O, 6.84
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| CAS # |
1049747-87-6
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| Related CAS # |
SB 242084; 181632-25-7
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| Appearance |
Solid powder
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| SMILES |
CC1=CC2=C(C=C1Cl)N(CC2)C(=O)NC3=CN=C(C=C3)OC4=C(N=CC=C4)C.Cl.Cl
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| InChi Key |
GCMNSEILNIPNSX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19ClN4O2.2ClH/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27);2*1H
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| Chemical Name |
6-chloro-5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-2,3-dihydroindole-1-carboxamide;dihydrochloride
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| Synonyms |
SB-242084 HCl; SB 242084; SB242084; SB-242084
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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 (e.g. under nitrogen), 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 : ~100 mg/mL (~213.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.69 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 50.0 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: ≥ 5 mg/mL (10.69 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 50.0 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. View More
Solubility in Formulation 3: ≥ 5 mg/mL (10.69 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 | 2.1378 mL | 10.6888 mL | 21.3776 mL | |
| 5 mM | 0.4276 mL | 2.1378 mL | 4.2755 mL | |
| 10 mM | 0.2138 mL | 1.0689 mL | 2.1378 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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