| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Multiple antagonistic effects of SB 242084 (100 nM; 45 min) on the increase in phosphatidylinositol workstation of 5-HT in human 5-HT2C workstation in SH-SY5Y cells have been reported [1]. SB 242084 (1–100 Nm; twenty-four hours)
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| ln Vivo |
In social interaction tests, SB 242084 (0.1–1 mg/kg; i.p.; single dosage; 20 min pretest) improves behavior [1]. SB 242084 (160-640 μg/kg; IV; single dose) dose-dependently and significantly increases basal current rates in dopaminergic neurons in the VTA (ventral tegmental area), as well as intrabody (DOPAC) levels. SB 242084 (5 mg/kg; i.p.; single dose; 20 minutes) SB 242084 (5, 10 mg/kg; i.p.; single dose) increases basal dialysate dopamine (DA) and hexaphenyl forms in the nucleus accumbens [ 3]. The same region also experiences increased burst activity [3].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SH-SY5Y cells Tested Concentrations: 100 nM Incubation Duration: 45 min Experimental Results: Antagonizes 5-HT-induced concentration-related increase) Increases RPTC in RPTC Respiration and PGC-1α mRNA expression [2]. In PI hydrolysis. RT-PCR[2] Cell Types: RPTC Cell Tested Concentrations: 1-100 nM Incubation Duration: 24 hrs (hours) Experimental Results: FCCP uncouples respiration and increases PGC-1α mRNA expression. |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) (CD) rat [1].
Doses: 0.1-1 mg/kg Route of Administration: intraperitoneal (ip) injection; single; 20 minutes Pre-test Experimental Results: Rats spent Dramatically more time in social interactions over 15 minutes under bright light conditions and in unfamiliar test boxes. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) (CD) rats (mCPP-induced Hypophagia model) [1]. Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; single; 20-minute pre-test Experimental Results: 23 hrs (hrs (hours)) of food deprivation during a 1-hour test period from the date of food presentation The amount of food consumed by rats was Dramatically diminished. Animal/Disease Models: Rat [2]. Doses: 5, 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Single Experimental Results:Basal dialysate dopamine (DA) and diamine in the nucleus accumbens Hydroxyphenylacetic acid (DOPAC) was Dramatically increased. |
| References |
[1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
[2]. Harmon JL, et al. 5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists. J Pharmacol Exp Ther. 2016 Apr;357(1):1-9. |
| Molecular Formula |
C21H19N4O2CL.2[HCL]
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|---|---|
| Molecular Weight |
467.77604
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| CAS # |
181632-25-7
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| Related CAS # |
SB 242084 dihydrochloride;1049747-87-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3
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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 : ≥ 44 mg/mL (~111.43 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.33 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 (6.33 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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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