S1PR5-IN-1
Based on 1 Customer Validation
S1PR5-IN-1 (Compound 7a) is a highly selective S1PR5 antagonist and orally bioavailable inhibitor with a human S1PR5 IC50 of 85.4 nM and human S1PR5 Kd of 2.173 nM.S1PR5-IN-1 binds to S1PR5 and inhibits natural killer cell migration toward sphingosine-1-phosphate.S1PR5-IN-1 can be used for the research of multiple sclerosis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.58%
- CAS. Nr.: 3107268-28-7
- Formel: C27H36FNO3
- Molecular Weight:441.58
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
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S1PR5 85.4 nM (IC50) |
S1PR4 >1000 nM (IC50) |
S1PR3 >1000 nM (IC50) |
S1PR2 >1000 nM (IC50) |
S1PR1 >1000 nM (IC50) |
In Vitro
[18F]S1PR5-IN-1 (Compound 7a) (0.02-33 nM) binds specifically and with high affinity to recombinant human S1PR5 cell membranes, with a Kd of 2.173 nM[1].
[18F]S1PR5-IN-1 (6.25-800 nM; 45 min) binds specifically to S1PR5 in C57BL/6 mouse brain tissue, with a Kd of 4.6 nM and a Bmax of 427.2 fmol/mg[1].
[18F]S1PR5-IN-1 (6.25-800 nM; 45 min) binds specifically to S1PR5 in post-mortem human cerebral cortex tissue, with a Kd of 27.6 nM and a Bmax of 381.6 fmol/mg[1].
[18F]S1PR5-IN-1 (~370 kBq per slide; 1 h) shows significantly reduced binding in brain sections from cuprizone-fed C57BL/6J mice compared to controls, reflecting decreased S1PR5 expression associated with demyelination[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
[18F]S1PR5-IN-1 (~15-22 MBq; i.v.; single injection) exhibits specific in vivo binding to S1PR5 in healthy male C57BL/6 mouse brains, as demonstrated by altered uptake following pretreatment with S1PR5 modulators (4 mg/kg; i.v.; 5 min pre-injection)[1].
[18F]S1PR5-IN-1 (~15-22 MBq; i.v.; single injection) detects reduced S1PR5 expression associated with cuprizone-induced demyelination in female C57BL/6J mice, with a 22.0% reduction in whole-brain SUV compared to control mice[1].
[18F]S1PR5-IN-1 (~158 MBq; i.v.; single injection) demonstrates rapid, high brain uptake and sustained retention in healthy male rhesus macaques, with regional uptake matching known primate S1PR5 expression patterns[1].
[18F]S1PR5-IN-1 (~44.4 MBq (rat), ~0.13 GBq (macaque); i.v.; single injection) exhibits high metabolic stability in healthy rats and rhesus macaques, with no brain-penetrant radiometabolites detected in either species[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3107268-28-7
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Appearance Solid
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Molecular Weight 441.58
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Formel C27H36FNO3
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Color White to off-white
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SMILES
CC(C)([C@@H]1CC[C@@H](OC2=CC(F)=C3C(C=CC=C3)=C2CN4CCC(CC4)C(O)=O)CC1)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 14.29 mg/mL (32.36 mM; ultrasonic and adjust pH to 4 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2646 mL | 11.3230 mL | 22.6460 mL | 56.6149 mL |
| 5 mM | 0.4529 mL | 2.2646 mL | 4.5292 mL | 11.3230 mL | |
| 10 mM | 0.2265 mL | 1.1323 mL | 2.2646 mL | 5.6615 mL | |
| 15 mM | 0.1510 mL | 0.7549 mL | 1.5097 mL | 3.7743 mL | |
| 20 mM | 0.1132 mL | 0.5661 mL | 1.1323 mL | 2.8307 mL | |
| 25 mM | 0.0906 mL | 0.4529 mL | 0.9058 mL | 2.2646 mL | |
| 30 mM | 0.0755 mL | 0.3774 mL | 0.7549 mL | 1.8872 mL |
S1PR5-IN-1 Related Classifications
HY-176533 Related Classifications
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