PW507
PW507 is a potent, brain-penetrant and selective sigma 1 receptor (S1R) antagonist with a Ki of 7.5 nM for human S1R. PW507 displays a low binding affinity to S2R and hERG. PW507 can be used for the study of painful diabetic neuropathy (PDN).
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- CAS No.: 2573850-59-4
- Formule: C18H27ClN4
- Masse moléculaire:334.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
PW507 binds to the orthosteric site of the human S1R crystal structure and engages in strong interactions with the receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PW507’s Pharmacokinetic Properties in SD rats Studies[1].
| plasma PK | IV | PO | IP |
| dose (mg/kg) | 1 | 25 | 10 |
| tmax (h) | N/A | 1.20 | 0.25 |
| t1/2 (h) | 0.53 | 0.69 | 0.56 |
| Cmax (ng/mL) | 193 | 296 | 671 |
| AUC0-inf (h*ng/mL) | 108 | 692 | 552 |
| CL (mL/min/kg) | 155 | N/A | N/A |
| ratio (brain/plasma, t = 0.25 h) | N/A | N/A | 12 |
| F (%) | 100 | 28 | 51 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SD rats injected Streptozotocin (HY-13753; STZ; 60 mg/kg)[1]
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Dosage:20 mg/kg
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Administration:i.p; twice daily; for 14 days
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Result:Demonstrated significant efficacy in alleviating mechanical allodynia hyperalgesia.
Chemical Information
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CAS No. 2573850-59-4
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Masse moléculaire 334.89
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Formule C18H27ClN4
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SMILES
CC(C)(C)C1=CC=C(C2=NC(CN3CCCC3)=NN2C)C=C1.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PW507 Related Classifications
HY-161873 Related Classifications
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