ARC 239 dihydrochlorideCAS: 67339-62-2
MF: C24H29N3O3•2HCl•xH2O
MW: 480.43
A selective α2B-AR adrenoreceptor antagonist.

ARC 239 dihydrochloride (CAS 67339-62-2)

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Application: A selective α2B-AR adrenoreceptor antagonist
CAS Number: 67339-62-2
Purity: ≥98%
Molecular Weight: 480.43
Molecular Formula: C24H29N3O32HCl•xH2O
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* Refer to Certificate of Analysis for lot specific data (including water content).
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ARC 239 dihydrochloride hydrate is a selective α2B-AR adrenoceptor antagonist with a pKD value of 8.8. This antagonist is known to display inhibitory effects on α2A-AR (α2A) and α2D receptors with pKD values of 6.7 and 6.4 respectively. Studies indicate that ARC 239 dihydrochloride is 100-fold more selective towards the α2B-AR (α2B adrenoceptor) than chlorpromazine (sc-357313) and 7-hydroxychlorpromazine. Studies conducted on pentobarbital-treated dogs and rats show that ARC 239 dihydrochloride competitively antagonizes pressor responses to adrenaline, while inhibiting these pressor responses to noradrenaline, phenylephrine, tyramine, and dimethylphenylpiperazinium. ARC 239 dihydrochloride hydrate is an inhibitor of α2B-AR.


References

1. Mouillé, P., et al. 1980. J. Cardiovasc. Pharmacol. 2: 175-191. PMID: 6171685
2. Bylund, D.B., et al. 1988. J.Pharmacol. Exp. Ther. 245: 600-607. PMID: 2835476

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and water (100 mM).
Storage :
Store at 4° C
Refractive Index :
n20D 1.58 (Predicted)
Ki Data :
α1A-AR: Ki= 1 nM (human); α2C-AR: Ki= 10 nM (human); α2B-AR: Ki= 10 nM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
10345075
MDL Number :
MFCD16875414
SMILES :
CC1(C2=CC=CC=C2C(=O)N(C1=O)CCN3CCN(CC3)C4=CC=CC=C4OC)C.Cl.Cl.O

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Certificate of Analysis

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