2. Neuronal Signaling
  3. Sigma Receptor
  4. 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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PW507 Chemical Structure

PW507 Chemical Structure

CAS No. : 2573850-59-4

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PW507 Related Antibodies

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Description

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)[1].

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.

PW507 Related Antibodies
In Vivo

PW507 (20 mg/kg; i.p; twice daily; for 14 days) demonstrates significant efficacy in alleviating mechanical allodynia hyperalgesia[1].
PW507’s Pharmacokinetic Properties in SD rats Studies[1].
1.19

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.

Animal Model: Male SD rats injected Streptozotocin (HY-13753; STZ; 60 mg/kg)[1]
Dosage: 20 mg/kg
Administration: i.p; twice daily; for 14 days
Result: Demonstrated significant efficacy in alleviating mechanical allodynia hyperalgesia.
Molecular Weight

334.89

Formula

C18H27ClN4
CAS No.
SMILES

CC(C)(C)C1=CC=C(C2=NC(CN3CCCC3)=NN2C)C=C1.Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PW507 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PW5072573850-59-4PW 507PW-507Sigma ReceptorS1R antagonistpainful diabetic neuropathybrain-penetrantInhibitorinhibitorinhibit

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