2573850-59-4

Name	1H-1,2,4-Triazole, 5-[4-(1,1-dimethylethyl)phenyl]-1-methyl-3-(1-pyrrolidinylmethyl)-, hydrochloride (1:1)
CAS	2573850-59-4
Molecular Formula	C18H26N4.ClH
Molecular Weight	334.89
MOL File	2573850-59-4.mol

Synonyms

1H-1,2,4-Triazole, 5-[4-(1,1-dimethylethyl)phenyl]-1-methyl-3-(1-pyrrolidinylmethyl)-, hydrochloride (1:1)

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Hazard Information

Uses

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 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
t_max (h)	N/A	1.20	0.25
t_1/2 (h)	0.53	0.69	0.56
C_max (ng/mL)	193	296	671
AUC_0-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

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.

References

[1] Youyi Peng, et al. Preclinical Evaluation of Sigma 1 Receptor Antagonists as a Novel Treatment for Painful Diabetic Neuropathy. ACS Pharmacol. Transl. Sci. July 18, 2024.

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