An α2-adrenergic receptor agonist
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Labeled Version(s)
30143Guanfacine-13C,15N3
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Guanfacine (hydrochloride)

Item No. 22907

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(aminoiminomethyl)-2,6-dichloro-benzeneacetamide, monohydrochloride
CAS Number
29110-48-3
Molecular Formula
C9H9Cl2N3O • HCl
Formula Weight
282.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 25 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
ClC1=C(CC(NC(N)=N)=O)C(Cl)=CC=C1.Cl
InChi Code
InChI=1S/C9H9Cl2N3O.ClH/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13;/h1-3H,4H2,(H4,12,13,14,15);1H
InChi Key
DGFYECXYGUIODH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $54

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    25 mg

    $120

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    50 mg

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    Product Description

    Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1 It has EC50 values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki = 19 nM in a radioligand binding assay).2 Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3 It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4 Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jasper, J.R., Lesnick, J.D., Chang, L.K., et al. Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS binding. Biochem. Pharmacol. 55(7), 1035-1043 (1998).

    2. Nikolic, K., Filipic, S., and Agbaba, D. QSAR study of imidazoline antihypertensive drugs. Bioorg. Med. Chem. 16(15), 7134-7140 (2008).

    3. Scholtysik, G. Pharmacology of guanfacine. Br. J. Clin. Pharmacol. 10(Suppl 1), 21S-24S (1980).

    4. Kauser, H., Sahu, S., Kumar, S., et al. Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive decline. Neuroscience 254, 110-119 (2013).