BRL-52537 hydrochloride
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 574338

CAS#: 112282-24-3

Description: BRL-52537 hydrochloride is a potent and highly selective κ-opioid agonist. It has neuroprotective effects in animal studies, and is used for research into potential treatments for stroke and heart attack as well as more general brain research.


Chemical Structure

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BRL-52537 hydrochloride
CAS# 112282-24-3

Theoretical Analysis

MedKoo Cat#: 574338
Name: BRL-52537 hydrochloride
CAS#: 112282-24-3
Chemical Formula: C18H25Cl3N2O
Exact Mass: 390.10
Molecular Weight: 391.760
Elemental Analysis: C, 55.19; H, 6.43; Cl, 27.15; N, 7.15; O, 4.08

Price and Availability

Size Price Availability Quantity
10mg USD 275 2 Weeks
50mg USD 830 2 Weeks
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Synonym: BRL-52537 hydrochloride; BRL-52537 HCl

IUPAC/Chemical Name: 2-(3,4-Dichlorophenyl)-1-[2-(1-pyrrolidinylmethyl)-1-piperidinyl]ethanone hydrochloride

InChi Key: NGVLSOWJSUUYDE-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H24Cl2N2O.ClH/c19-16-7-6-14(11-17(16)20)12-18(23)22-10-2-1-5-15(22)13-21-8-3-4-9-21;/h6-7,11,15H,1-5,8-10,12-13H2;1H

SMILES Code: ClC1=CC=C(CC(N2C(CN3CCCC3)CCCC2)=O)C=C1Cl.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: Potent and selective κ agonist.
In vitro activity: TBD
In vivo activity: Adult male Sprague-Dawley rats were randomly assigned into sham (group A), I/R (group B), BRL52537 (KOR agonist) + I/R (group C), nor-BNI (nor-binaltorphimine, KOR antagonist) + I/R (group D), AG490 (STAT3 phosphorylation inhibitor) + I/R (group E), dimethyl sulfoxide (DMSO, vehicle of AG490) + I/R (group F), and BRL52537 + AG490 +I/R (group G) groups. Cerebral I/R injury was induced by 10 min exposure to global ischemia (4-VO). Results showed that BRL52537 protects against I/R injury-induced brain damage and inhibits neuronal apoptosis to a significant extent. Additionally, BRL52537 promoted up-regulation of p-STAT3 and a marked decrease in caspase-3 expression. Reference: Neurochem Res. 2013 Nov;38(11):2305-12. https://pubmed.ncbi.nlm.nih.gov/23996400/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Water 2.0 5.00

Preparing Stock Solutions

The following data is based on the product molecular weight 391.76 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Fang S, Xu H, Lu J, Zhu Y, Jiang H. Neuroprotection by the kappa-opioid receptor agonist, BRL52537, is mediated via up-regulating phosphorylated signal transducer and activator of transcription-3 in cerebral ischemia/reperfusion injury in rats. Neurochem Res. 2013 Nov;38(11):2305-12. doi: 10.1007/s11064-013-1139-4. Epub 2013 Aug 31. PMID: 23996400. 2. Zeynalov E, Nemoto M, Hurn PD, Koehler RC, Bhardwaj A. Neuroprotective effect of selective kappa opioid receptor agonist is gender specific and linked to reduced neuronal nitric oxide. J Cereb Blood Flow Metab. 2006 Mar;26(3):414-20. doi: 10.1038/sj.jcbfm.9600196. PMID: 16049424.
In vitro protocol: TBD
In vivo protocol: 1. Fang S, Xu H, Lu J, Zhu Y, Jiang H. Neuroprotection by the kappa-opioid receptor agonist, BRL52537, is mediated via up-regulating phosphorylated signal transducer and activator of transcription-3 in cerebral ischemia/reperfusion injury in rats. Neurochem Res. 2013 Nov;38(11):2305-12. doi: 10.1007/s11064-013-1139-4. Epub 2013 Aug 31. PMID: 23996400. 2. Zeynalov E, Nemoto M, Hurn PD, Koehler RC, Bhardwaj A. Neuroprotective effect of selective kappa opioid receptor agonist is gender specific and linked to reduced neuronal nitric oxide. J Cereb Blood Flow Metab. 2006 Mar;26(3):414-20. doi: 10.1038/sj.jcbfm.9600196. PMID: 16049424.

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