1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor Vasopressin Receptor
  3. AGN-190851

AGN-190851 is a potent and selective agonist of α2-adrenergic receptor (α2 adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α2-adrenergic receptor subtypes, and parturition.

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AGN-190851

AGN-190851 Chemical Structure

CAS No. : 134892-42-5

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Description

AGN-190851 is a potent and selective agonist of α2-adrenergic receptor (α2 adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α2-adrenergic receptor subtypes, and parturition[1][2].

IC50 & Target[1]

Alpha-2A adrenergic receptor

 

V2 Receptor 

 

In Vitro

AGN-190851 dose-dependently inhibits vasopressin-stimulated cyclic AMP accumulation in rat cortical collecting tubules in vitro, but does not inhibit vasopressin-stimulated adenylate cyclase activity in dog cortical collecting tubules in vitro[1].

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

In Vivo

AGN-190851 induces dose-dependent water diuresis in rats in vivo, but produces no significant diuretic or renal functional effects in conscious dogs and anesthetized cynomolgus monkeys[1].
AGN-190851 (0.06-0.1 mg/kg; i.m.; single dose administered 20 h after intramuscular PGF2α 10 mg/sow) combined with prostaglandin F2α reduces the interval from treatment to farrowing in pregnant sows[2].

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

Animal Model: Landrace-Yorkshire sows (2 to 13 parities, mean 5.2 parities; 170 to 270 kg, mean 206 kg)[2]
Dosage: 0.06 mg/kg; 0.1 mg/kg
Administration: i.m.; single dose (administered 20 h after intramuscular prostaglandin F2α 10 mg/sow)
Result: Reduced the mean interval from second treatment to farrowing to 3.0 h at 0.06 mg/kg and 2.1 h at 0.1 mg/kg.
Lowered the mean stillbirth rate to 12.1% at 0.06 mg/kg and 3.9% at 0.1 mg/kg.
Required manual farrowing assistance in 2/20 sows at 0.06 mg/kg and 3/20 sows at 0.1 mg/kg.
Induced vomiting in 7/20 sows at 0.06 mg/kg and 11/20 sows at 0.1 mg/kg.
Molecular Weight

296.17

Formula

C11H14BrN5

CAS No.
SMILES

BrC1=C2NCCNC2=CC=C1/N=C3NCCN/3

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

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AGN-190851
Cat. No.:
HY-165456
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