| 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 |
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Purity: ≥98%
| ln Vitro |
In rat striatal membranes, SCH442416 is more selective for A2AR (Ki=0.50 nM) than for A1R and A3R (Ki 1815 and >10000, respectively) [1]. In Müller cells, SCH442416 (0.1-10 μM) increases the expression of the proteins glutamine synthetase (GS) and glutamate aspartate transporter (GLAST) in group 1 μM [5].
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| ln Vivo |
SCH-442416 (0.017 mg/kg; i.p.) totally reversed CGS-21680-induced reduction in skeletal muscle damage [3]. Rats' expression of the GS and GLAST proteins is elevated by SCH-442416 (1 μM·2μL; iv) [5]. Adenosine-induced dilation is greatly attenuated (from 15.3 μm to 5.6 μm) by SCH442416 (1 μM) [4].
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| References |
[1]. Todde S, et, al. Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography. J Med Chem. 2000 Nov 16;43(23):4359-62.
[2]. Moresco RM, et, al. In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416. Eur J Nucl Med Mol Imaging. 2005 Apr;32(4):405-13. [3]. Zheng J, et, al. Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am J Physiol Heart Circ Physiol. 2007 Dec;293(6):H3685-91. [4]. Maimon N, et, al. Pre-exposure to adenosine, acting via A(2A) receptors on endothelial cells, alters the protein kinase A dependence of adenosine-induced dilation in skeletal muscle resistance arterioles. J Physiol. 2014 Jun 15;592(12):2575-90. [5]. Yu J, et, al. A 2A R Antagonists Upregulate Expression of GS and GLAST in Rat Hypoxia Model. Biomed Res Int. 2020 Oct 26;2020:2054293. |
| Additional Infomation |
LSM-3027 is a member of triazolopyrimidines.
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| Molecular Formula |
C20H19N7O2
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|---|---|
| Molecular Weight |
389.42
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| Exact Mass |
389.16
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| CAS # |
316173-57-6
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| PubChem CID |
10668061
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| Appearance |
Off-white to light brown solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.752
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| LogP |
2.75
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(CCCN2C3=C(C=N2)C4=NC(=NN4C(=N)N3)C5=CC=CO5)C=C1
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| InChi Key |
AEULVFLPCJOBCE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N7O2/c1-28-14-8-6-13(7-9-14)4-2-10-26-18-15(12-22-26)19-23-17(16-5-3-11-29-16)25-27(19)20(21)24-18/h3,5-9,11-12H,2,4,10H2,1H3,(H2,21,24)
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| Chemical Name |
4-(furan-2-yl)-10-[3-(4-methoxyphenyl)propyl]-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 |
SCH442416; SCH 442416; SCH-442416
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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 : ~62.5 mg/mL (~160.50 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 0.2 mg/mL (0.51 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 2.0 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: ≥ 0.2 mg/mL (0.51 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 2.0 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 | 2.5679 mL | 12.8396 mL | 25.6792 mL | |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1358 mL | |
| 10 mM | 0.2568 mL | 1.2840 mL | 2.5679 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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