1. GPCR/G Protein
    Neuronal Signaling
  2. Sigma Receptor
  3. S1RA hydrochloride

S1RA hydrochloride (Synonyms: E-52862 hydrochloride)

Cat. No.: HY-18099A Purity: 99.24%
Handling Instructions

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

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

S1RA hydrochloride Chemical Structure

S1RA hydrochloride Chemical Structure

CAS No. : 1265917-14-3

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10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 165 In-stock
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25 mg USD 350 In-stock
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50 mg USD 550 In-stock
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100 mg USD 950 In-stock
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250 mg USD 1950 In-stock
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Description

S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM). IC50 value: 17 nM (Ki) [1] Target: σ1R antagonist in vitro: S1RA behaved as a highly selective σ1 receptor antagonist. It showed high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). Moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) was found at the human 5-HT2B receptor. S1RA showed no significant affinity (Ki > 1 μM or % inhibition at 1 μM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes) [2]. in vivo: Control (non-operated) and nerve-injured mice received a single or repeated (twice daily for 12 days) i.p. administration of S1RA at 25 mg·kg 1, the same dose used for the assessment of behavioural hypersensitivity in the chronic treatment study. Acute treatment was given on day 12 post-surgery and repeated treatment with S1RA started the day of surgery, as in the behavioural studies [2]. Intrathecal pre-treatment with idazoxan prevented the systemic S1RA antinociceptive effect, suggesting that the S1RA antinociception depends on the activation of spinal α2 -adrenoceptors which, in turn, could induce an inhibition of formalin-evoked glutamate release. When administered locally, intrathecal S1RA inhibited only the flinching behavior, whereas intracerebroventricularly or intraplantarly injected also attenuated the lifting/licking behavior [3].

Molecular Weight

373.88

Formula

C₂₀H₂₄ClN₃O₂

CAS No.
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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (267.47 mM; Need ultrasonic)

H2O : 16.67 mg/mL (44.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6747 mL 13.3733 mL 26.7465 mL
5 mM 0.5349 mL 2.6747 mL 5.3493 mL
10 mM 0.2675 mL 1.3373 mL 2.6747 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 110 mg/mL (294.21 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.69 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
S1RA hydrochloride
Cat. No.:
HY-18099A
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