ChemicalBook > CAS DataBase List > S1RA (hydrochloride)

S1RA (hydrochloride)

Product Name: S1RA (hydrochloride)
CAS No.: 1265917-14-3
Chemical Name: S1RA (hydrochloride)
Synonyms: 177303;S1RA. HCL;S1RA HCl (E-52862);S1RA (E-52862) HCI;S1RA (hydrochloride);E52862 hydrochloride;E 52862 hydrochloride;E-52862 hydrochloride;S1RA hydrochloride, 10 mM in DMSO;E-52862 HYDROCHLORIDE;E52862 HYDROCHLORIDE;E 52862 HYDROCHLORIDE
CBNumber: CB72682021
Molecular Formula: C20H24ClN3O2
Formula Weight: 373.88
MOL File: 1265917-14-3.mol

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S1RA (hydrochloride) Property

storage temp.: -20°C (des.)
solubility: Soluble in DMSO (up to at least 25 mg/ml)
form: solid
color: Off-white
Stability:: Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene

Product number: CS-2188
Product name: S1RAhydrochloride
Purity: 99.24%
Packaging: 5mg
Price: $110
Updated: 2021/12/16

ChemScene

Product number: CS-2188
Product name: S1RAhydrochloride
Purity: 99.24%
Packaging: 10mg
Price: $165
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BS177543
Product name: S1RA hydrochloride
Packaging: 25mg
Price: $240
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BS177543
Product name: S1RA hydrochloride
Packaging: 50mg
Price: $320
Updated: 2021/12/16

ChemScene

Product number: CS-2188
Product name: S1RAhydrochloride
Purity: 99.24%
Packaging: 50mg
Price: $550
Updated: 2021/12/16

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S1RA (hydrochloride) Chemical Properties,Usage,Production

Description

S1RA (E-52862, 1265917-14-3) is a potent and selective σ1 antagonist with weak binding at σ2?(IC50?σ1 = 17nM, σ2 = 9300nM).1,2?S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ1 dependent manner.3?S1RA potentiated μ-opioid antinociception in mice in a σ-dependent manner.4?S1RA displayed neuroprotective effects in a mouse model of ischemic stroke.5

Uses

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization[1][2].

in vivo

S1RA hydrochloride (i.p. 16-80 mg/kg or oral administration 32-128 mg/kg; once) dose-dependently inhibits formalin-induced nociception, capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity of mice^[1].

Animal Model:	Male CD1 mice^[1]
Dosage:	32, 64, 128 and 160 mg/kg
Administration:	Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
Result:	Reduced the permanence time on the rotating rod in rotarod test.

Animal Model:	Male CD1 mice with formalin-evoked nociception^[1]
Dosage:	20, 40 and 80 mg/kg
Administration:	Intraperitoneal injection; 20, 40 and 80 mg/kg, once
Result:	Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.

Animal Model:	Male CD1 mice with capsaicin-induced mechanical hypersensitivity^[1]
Dosage:	16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration)
Administration:	Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once
Result:	Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.

IC 50

Sigma 1 Receptor

References

[1] SIEMENS H, ROODT V. References and Citations[C]. 2008: 0. DOI:10.1515/9783110217339.0.xiii

S1RA (hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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E52862 hydrochloride

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E-52862 HYDROCHLORIDE;E52862 HYDROCHLORIDE;E 52862 HYDROCHLORIDE

177303

S1RA (E-52862) HCI

S1RA HCl (E-52862)

Inhibitor,E 52862,S1RA hydrochloride,E52862,S1RA,E-52862,inhibit,S-1RA hydrochloride,Sigma Receptor

S1RA hydrochloride, 10 mM in DMSO

1265917-14-3

C20H23N3O2HCl