S1RA (E-52862) HCI

This product is for research use only, not for human use. We do not sell to patients.

S1RA (E-52862) HCI
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Cat #: V28975 CAS #: 1265917-14-3 (HCl) Purity ≥ 99%

Description: S1RA HCl (also known as E-52862 HCl) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).

References: Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306.

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Molecular Weight (MW)373.881
Molecular FormulaC20H24ClN3O2
CAS No.1265917-14-3 (HCl)
SynonymsE-52862 hydrochloride
ProtocolIn VitroS1RA hydrochloride (0.1-10000 nM) has Ki values of 17 and 23.5 nM for σ1R for humans and guinea pigs, respectively
In VivoS1RA hydrochloride (16-80 mg/kg intraperitoneally or 32-128 mg/kg orally; Once) dose-dependent inhibition of formalin-induced pain sensation, capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity in mice
Animal modelMale CD1 mice
Dosages32, 64, 128 and 160 mg/kg
AdministrationIntraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.6746 mL13.3732 mL26.7465 mL53.4930 mL
5mM0.5349 mL2.6746 mL5.3493 mL10.6986 mL
10mM0.2675 mL1.3373 mL2.6746 mL5.3493 mL
20mM0.1337 mL0.6687 mL1.3373 mL2.6746 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

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Volume(final)
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Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.