Structure of SCH58261
CAS No.: 160098-96-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
4.5
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 160098-96-4 |
Formula : | C18H15N7O |
M.W : | 345.36 |
SMILES Code : | NC1=NC(N(CCC2=CC=CC=C2)N=C3)=C3C4=NC(C5=CC=CO5)=NN14 |
MDL No. : | MFCD00933778 |
InChI Key : | UTLPKQYUXOEJIL-UHFFFAOYSA-N |
Pubchem ID : | 176408 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Hippocampal slices | 10 nM | 20 minutes | SCH58261 prevented the CX3CL1-induced potentiation of NMDA-fEPSPs, indicating that A2AR activity is crucial for CX3CL1-mediated modulation of NMDARs. | PMC3765929 |
N9 microglial cells | 50 nM | 6 hours | SCH58261 prevented the LPS-induced decrease of mBDNF, indicating that A 2AR plays a key role in LPS-induced BDNF secretion. | PMC3567964 |
Xenopus oocytes | 10 nM | SCH58261 reduced IGABA run-down in ∼40% of tested oocytes but increased it in ∼20% of tested oocytes. | PMC2567502 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | Spinal cord injury model | Intraperitoneal injection | 0.3 mg/kg DAC and 10 mg/kg TAK-243 | three times per week until recipient mice died | SCH58261 protects against spinal cord injury by acting on centrally located A2A receptors, likely reducing excitotoxicity. | PMC3096915 |
Mice | Head and neck squamous cell carcinoma (HNSCC) mouse model | Intraperitoneal injection | 50 mg/kg/day | Once daily for 16 days | SCH58261 significantly delayed tumor growth in the HNSCC mouse model and significantly reduced the population of CD4+Foxp3+ regulatory T cells, enhancing the anti-tumor response of CD8+ T cells | PMC5461710 |
BALB/c nu/nu mice | OSCC xenograft model | Intraperitoneal injection | 1 mg/kg | Every other day for 25 days | SCH58261 impeded the growth of OSCC xenograft by blocking trigeminal A2AR signaling and reduced the release of CGRP. | PMC11183250 |
C57BL/6 mice | IE9mp1-mIDO1 ovarian cancer model | Intraperitoneal injection | 50 mg/kg·d | From GD9 to GD18, once daily | To test whether the combination of IDO1 inhibitor and A2a/A2b receptor antagonists could improve the survival rate of ovarian cancer-bearing mice. The results showed that the combination of IDO1 inhibitor and A2a/A2b receptor antagonists significantly improved the survival rate of mice. | PMC9311231 |
Mice | Chronic unpredictable stress (CUS) model | Intraperitoneal injection | 5 mg/kg | Daily until the end of the experiment | SCH58261 treatment reversed the CUS-induced behavioral and synaptic dysfunction, restoring performance in the forced swimming test, elevated plus maze test, and modified Y maze test, and restored the density of synaptic markers and the amplitude of long-term potentiation (LTP) in the hippocampus. | PMC4485143 |
Mice | Experimental autoimmune encephalomyelitis (EAE) model | Intraperitoneal and subcutaneous injection | 1mg/kg | 5 days on, 2 days off, from day 7 to day 21 | To evaluate the protective effect of SCH58261 on EAE progression, results showed that SCH58261 significantly protected mice from EAE development | PMC2453691 |
C57BL/6 and BALB/c mice | Orthotopic liver tumor model | Intraperitoneal injection | 0.1 mg/kg | Once daily for 3 weeks | Combination of SCH58261 with anti-PD1 therapy showed stronger anti-tumor effects in orthotopic liver tumor models, while SCH58261 monotherapy was ineffective. | PMC10772255 |
Tags: SCH 58261 | SCH58261 | SCH-58261 | Adenosine Receptor | P1 receptor | A2A receptor antagonist | adenosine receptor | immune modulation | anti-inflammatory | 160098-96-4
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H260 | In contact with water releases flammable gases which may ignite spontaneously |
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Health hazards | |
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H304 | May be fatal if swallowed and enters airways |
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H310 | Fatal in contact with skin |
H311 | Toxic in contact with skin |
H312 | Harmful in contact with skin |
H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
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H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
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H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
H370 | Causes damage to organs |
H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
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H401 | Toxic to aquatic life |
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H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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