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EST73502 HCl

Catalog No. T39284   CAS 2307458-82-6

EST73502 is an agonist of μ-opioid receptor(Ki = 64 nM) agonist and an antagonist of σ1 receptor (Ki = 118 nM). EST73502 displays antinociceptive activity.

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EST73502 HCl Chemical Structure
EST73502 HCl, CAS 2307458-82-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 155.00
5 mg In stock $ 317.00
10 mg In stock $ 452.00
25 mg In stock $ 745.00
50 mg In stock $ 1,050.00
100 mg In stock $ 1,390.00
500 mg In stock $ 2,830.00
1 mL * 10 mM (in DMSO) In stock $ 346.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EST73502 is an agonist of μ-opioid receptor(Ki = 64 nM) agonist and an antagonist of σ1 receptor (Ki = 118 nM). EST73502 displays antinociceptive activity.
Targets&IC50 μ-opioid receptor:64 nM(Ki), δ-opioid receptor:118 nM(Ki)
In vivo In CD1 male mice, EST73502 (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC50 of 14 mg/kg in the paw pressure test. EST73502 (5 mg/kg; i.p.) attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%[1].
Molecular Weight 388.88
Formula C19H27ClF2N2O2
CAS No. 2307458-82-6

Storage

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

Solubility Information

DMSO: 50 mg/mL (128.57 mM)

TargetMolReferences and Literature

1. Mónica García, et al. Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ 1 Receptor Antagonist Clinical Candidate for the Treatment of Pain. J Med Chem. 2020 Oct 16.

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Keywords

EST73502 HCl 2307458-82-6 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor EST73502 EST-73502 inhibitor inhibit

 

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