| 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%
SCH-58261 (SCH58261; SCH 58261) is a novel, potent, selective and competitive antagonist of the adenosine A2A receptor with immunomodulatory and neuroprotective effects. Its Ki values for rat and bovine adenosine A2a are 2.3 nM and 2 nM, respectively, indicating its inhibition of these enzymes. SCH-58261 exhibits selectivity over A1, A2B, and A3 receptors that is 323-, 53-, and 100-fold, respectively. In a rat model of Parkinson's disease, 6-hydroxy dopamine-induced motor deficits have been ameliorated with SCH 58261. SCH 58261 was found to be effective in lowering the levels of demyelination, TNF-α, Fas-L, PAR, Bax expression, and JNK MAPK activation in a mouse model of spinal cord injury. It has been observed that ongoing SCH58261 treatment improves the neurological deficit.
| Targets |
bovine A2a ( Ki = 2.0 nM ); rat A2a ( Ki = 2.3 nM )
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Male Sprague-Dawley rats weighing 250–300 g are used to harvest the cortex and striatum of the rat brain. Within 10 mm after an animal is sacrificed, the frontal cortex and striatum of cow brains are taken from a nearby abattoir. [3H]CHA and [3H]CGS 21680 are used in the A1 and A2a ADO receptor binding assays. (3H) 2-[4-phenethylamino]-(2-carboxyethyl) as radioligands, 5'-N-ethylcarboxamidoadenosinel in this case. Using [125I]AB-MECA as the radioligand, a binding assay is carried out on CHO cells that have been stable transfected with the rat brain A3 ADO receptor. Saturation experiments are performed on rat brain tissues in the absence or presence of varying concentrations of SCH 58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]) in order to ascertain the type of inhibition (competitive or noncompetitive) at A1 ADO ([3H]CHA, 0.125-64 nM) and A2a ADO receptors ([3HJCGS 21680, 1-128 aM).[1,5-c]triazolo[1,2,4-]pyrimidine}. SCH 58261's affinity for a number of neurotransmitter binding sites, including mu-opioid, benzodiazepine, N-methyl-D-aspartate, D1 and D2 dopamine receptors, 5-HT1 and 5-HT2 receptors, M1 and M2 muscarinic receptors, and alpha-1, alpha-2, and beta-1 adrenoceptors, is determined using standard procedures.
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| Cell Assay |
In the NSCLC cell line H1975, SCH 58261 reduces cell viability in a concentration-dependent manner.
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| Animal Protocol |
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| References |
| Molecular Formula |
C18H15N7O
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| Molecular Weight |
345.36
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| Exact Mass |
345.13
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| Elemental Analysis |
C, 62.60; H, 4.38; N, 28.39; O, 4.63
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| CAS # |
160098-96-4
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C=C1)CCN2C3=C(C=N2)C4=NC(=NN4C(=N3)N)C5=CC=CO5
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| InChi Key |
UTLPKQYUXOEJIL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15N7O/c19-18-22-16-13(11-20-24(16)9-8-12-5-2-1-3-6-12)17-21-15(23-25(17)18)14-7-4-10-26-14/h1-7,10-11H,8-9H2,(H2,19,22)
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| Chemical Name |
4-(furan-2-yl)-10-(2-phenylethyl)-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-7-amine
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.02 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 20.8 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: ≥ 2.08 mg/mL (6.02 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 4%DMSO + 40%PEG300 + 4%Tween 80 52%ddH2O: 2.0mg/ml (5.79mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8955 mL | 14.4776 mL | 28.9553 mL | |
| 5 mM | 0.5791 mL | 2.8955 mL | 5.7911 mL | |
| 10 mM | 0.2896 mL | 1.4478 mL | 2.8955 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.
Effect of caffeine (10 and 30 mg/kg, i.p.) and SCH58261 (2mg/kg, i.p.) on normal rats 10, 30 and 60 min after administration in beam test.Acta Cir Bras.2016 Feb;31(2):133-7. |
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Effect of caffeine (10 and 30 mg/kg, i.p.) and SCH58261 (2mg/kg, i.p.) on 6OHDA-lesioned rats 10, 30 and 60 min after administration in beam test.Acta Cir Bras.2016 Feb;31(2):133-7. |
The results of beam test in normal, sham-operated and 6-OHDA (8 μg/2μL/rat) lesioned rats.Acta Cir Bras.2016 Feb;31(2):133-7. |
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