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EST73502 monohydrochloride - 10mM in DMSO, high purity , CAS No.2535970-65-9(DMSO)

  • 10mM in DMSO
Item Number
E655426
Grouped product items
SKUSizeAvailabilityPrice Qty
E655426-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$440.90

Basic Description

Specifications & Purity10mM in DMSO
Storage TempDesiccated,Store at -80°C
Shipped InIce chest + Ice pads
Product Description

EST73502 monohydrochloride 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 monohydrochloride has antinociceptive activity

In Vivo

EST73502 monohydrochloride (10-40 mg/kg; p.o.) shows a dose-response analgesic effect reaching a maximum of 64% and an EC 50 of 14 mg/kg in the paw pressure test in CD1 male mice . EST73502 monohydrochloride (5 mg/kg; i.p.; twice a day; for 10 days) attenuates partial sciatic nerve ligation (PSNL)-induced mechanical allodynia in male CD1 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD1 mice, PSNL model 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%.

IC50& Target:Ki: 64 nM (MOR), 118 nM (σ1R)

Names and Identifiers

Canonical SMILES CCN1CC2(CCN(CC2)CCC3=C(C=CC(=C3)F)F)OC(C1=O)C.Cl
Molecular Weight 388.88

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