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EST73502 hydrochloride

Catalog No. T9669   CAS 2535970-65-9

EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity with reduced opioid-induced relevant adverse events[1].

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EST73502 hydrochloride Chemical Structure
EST73502 hydrochloride, CAS 2535970-65-9
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 228.00
25 mg 6-8 weeks $ 1,400.00
50 mg 6-8 weeks $ 1,820.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with K i s of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity with reduced opioid-induced relevant adverse events[1].
In vivo EST73502 hydrochloride administered orally (10-40 mg/kg) demonstrates a dose-dependent analgesic effect, achieving a peak reduction in pain of 64% with an Effective Concentration (EC 50) of 14 mg/kg in the paw pressure test on CD1 male mice [1]. Additionally, intraperitoneal injections of EST73502 hydrochloride (5 mg/kg; twice daily for 10 days) significantly mitigate mechanical allodynia caused by partial sciatic nerve ligation (PSNL) in these mice, showing a maximum efficacy of 56% [1]. This is observed in the same CD1 male mouse model using PSNL to simulate the condition [1].
Molecular Weight 388.88
Formula C19H27ClF2N2O2
CAS No. 2535970-65-9

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

EST73502 hydrochloride 2535970-65-9 EST73502 Hydrochloride EST-73502 Hydrochloride EST 73502 Hydrochloride inhibitor inhibit

 

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