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  3. EST73502 hydrochloride

EST73502 hydrochloride 

Cat. No.: HY-134189A Purity: 98.12% ee.: 100.0%
Handling Instructions

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 Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity.

For research use only. We do not sell to patients.

EST73502 hydrochloride Chemical Structure

EST73502 hydrochloride Chemical Structure

CAS No. : 2535970-65-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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 Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity[1].

IC50 & Target

Ki: 64 nM (MOR), 118 nM (σ1R)[1]

In Vivo

EST73502 hydrochloride (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 in CD1 male mice[1].
EST73502 hydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male CD1 mice, PSNL model[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, twice a day, for 10 days
Result: Attenuated the expression of mechanical allodynia induced by PSNL, reaching a maximal effect of 56%.
Molecular Weight

388.88

Formula

C₁₉H₂₇ClF₂N₂O₂

CAS No.

2535970-65-9

SMILES

FC1=CC=C(F)C=C1CCN(CC2)CCC2(O[[email protected]@H]3C)CN(CC)C3=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

EST73502EST 73502EST-73502Sigma ReceptorOpioid ReceptoranalgesicacutechronicpainantinociceptionInhibitorinhibitorinhibit

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Product Name:
EST73502 hydrochloride
Cat. No.:
HY-134189A
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