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S1R antagonist

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SI-6271

S1R antagonist, >98% (HPLC)

CAS No. : [1353916-16-9]

IUPAC Name : 5-(4-(Tert-butyl)phenyl)-1-methyl-3-(pyrrolidin-1-ylmethyl)-1H-1,2,4-triazole

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Chemical Properites
Mol. Formula :
C18H26N4
Mol. Weight :
298.43
Appearance :
Solid
Melting Point :
Not available
For Laboratory research use only, not for drug, household or other uses.

Applications : This is a potent and highly selective sigma‑1 receptor (S1R) antagonist from a triazole‑based series, showing strong S1R affinity, high selectivity over S2R and 87 other targets, and good metabolic stability with slow microsomal clearance. It also demonstrates excellent BBB permeability in rats. In vivo, it shows no acute toxicity and produces significant analgesic effects in both formalin‑induced inflammatory pain and paclitaxel‑induced neuropathic pain models, supporting its promise as a novel S1R‑targeted analgesic for diverse pain conditions.

References : Peng Y. et al.: J. Med. Chem., 64(2), 890-904, 2021.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.

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