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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
25mg
Price
$350
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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S1RA (hydrochloride) Suppliers

China 50 United States 9 Global 59
Shanghai Boyle Chemical Co., Ltd.
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China
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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info@chemexpress.com
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MedChemexpress LLC
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021-58955995
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609-228-5909
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sales@medchemexpress.cn
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Shanghai JiYi Biotechnology Co. Ltd.
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13621943973
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sales@shjiyipharmatech.com
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SPIRO PHARMA
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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021-65675885
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Guangzhou QiYun Biotechnology Co., Ltd.
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020-61288194 61288195
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020-61288700
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505721671@qq.com
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Tianjin Kailiqi Biotechnology Co., Ltd.
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15076683720
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022-23754520
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klq@cw-bio.com
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Amadis Chemical Company Limited
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571-89925085
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0086-571-89925065
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sales@amadischem.com
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Shanghai Biopharmaleader Co., Ltd.
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+86 18721201413
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+86 (21) 5775-8967
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