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
- 화학식: C18H27ClN4
- 분자량:334.89
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Sigma Receptor Isoforms
More
Biological Activity
제품 설명
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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분자량 334.89
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화학식 C18H27ClN4
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SMILES
CC(C)(C)C1=CC=C(C2=NC(CN3CCCC3)=NN2C)C=C1.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)