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Cat. No.: HY-103216A

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RWJ52353 hydrochloride

RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC₅₀s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport.

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

CAS No.: 245744-13-2
Formula: C₁₁H₁₁ClN₂S
Molecular Weight:238.74

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

RWJ52353 hydrochloride Chemical Structure

CAS No.: 245744-13-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Ki: 1.5 nM (α_2D AR), 254 nM (α_2A AR), 621 nM (α_2B AR), 443 nM (α₁ AR)^[1]
IC50: 100 μM (rOCT1), 20 μM (rOCT2)^[2]

All Adrenergic Receptor Isoforms :

In Vivo

RWJ-52353 (30 mg/kg; po; single dose) hydrochloride has an inhibitory effect on the induced abdominal pain model in mice, with an inhibition rate of 100%^[1].
RWJ-52353 The ED50s in the mouse abdominal pain model are 15.1 mg/kg (po) and 11.6 mg/kg (po) respectively^[1].
RWJ-52353 can also reduce the risk of mice in the hot plate test (48°C) and shaking The degree of pain in the tail experiment, ED50s are 25.9 mg/kg (po) and 100.2 mg/kg (po) respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 245744-13-2
Molecular Weight 238.74
Formula C₁₁H₁₁ClN₂S
SMILES

C1(C2=CCCC3=C2C=CS3)=CN=CN1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ross T M, et al. α2 Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1, 3-dimethyl-6, 7-dihydrothianaphthene as a high-affinity ligand for the α2D adrenergic receptor[J]. Journal of medicinal chemistry, 2000, 43(7): 1423-1426.

[2]. Amphoux A, et al. Inhibitory and facilitory actions of isocyanine derivatives at human and rat organic cation transporters 1, 2 and 3: a comparison to human alpha 1- and alpha 2-adrenoceptor subtypes. Eur J Pharmacol. 2010 May 25;634(1-3):1-9. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References

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RWJ52353 hydrochloride

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

RWJ52353 hydrochloride Related Classifications

HY-103216A Related Classifications