1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Vemtoberant mesylate

Vemtoberant (APD418) mesylate is a β3-adrenergic receptor (β3-AR) antagonist with a human Ki of 8.2 nM, and exhibits 400- to 600-fold selectivity over human β1-AR and β2-AR. Vemtoberant mesylate attenuates β3-AR-mediated cardiac inhibition. Vemtoberant mesylate can be used for the research of systolic heart failure.

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Vemtoberant mesylate

Vemtoberant mesylate Chemical Structure

CAS No. : 2169905-97-7

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Description

Vemtoberant (APD418) mesylate is a β3-adrenergic receptor (β3-AR) antagonist with a human Ki of 8.2 nM, and exhibits 400- to 600-fold selectivity over human β1-AR and β2-AR. Vemtoberant mesylate attenuates β3-AR-mediated cardiac inhibition. Vemtoberant mesylate can be used for the research of systolic heart failure[1].

In Vivo

Vemtoberant (0.35-15.0 mg/kg/h; i.v.; continuous infusion) mesylate produces dose-dependent, sustained improvements in left ventricular systolic and diastolic function in dogs with systolic heart failure, with a 6-hour infusion at 0.70 mg/kg/h increasing LVEF by 7 percentage points and Ei/Ai by 1.5 units, without significant effects on heart rate or systemic blood pressure[1].

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

Animal Model: Mongrel dogs (healthy conditioned, weighing 19.9-30.6 kg, systolic heart failure model via serial intracoronary microembolizations)[1]
Dosage: 0.35 mg/kg/h; 0.70 mg/kg/h; 1.4 mg/kg/h; 2.8 mg/kg/h; 5.6 mg/kg/h; 10.0 mg/kg/h; 15.0 mg/kg/h
Administration: i.v.; continuous infusion
Result: Increased LVEF from 34% to 38%, decreased LV ESV from 41 mL to 38 mL, increased FAS from 34% to 37%, increased Ei/Ai from 3.1 to 3.6 at 1.4 mg/kg/h.
Increased LVEF to 41%, decreased LV ESV to 36 mL, increased FAS to 41%, increased Ei/Ai to 4.3, increased CO to 2.14L/min, decreased LVEDP to 12 mm Hg at 5.6 mg/kg/h.
Caused modest significant decreases in SVR and increases in DCT at 0.35 mg/kg/h .
Increased LVEF from 32% to 38%, decreased LV ESV from 35 mL to 32 mL, increased FAS from 33% to 38%, increased CO from 1.36 L/min to 1.62 L/min, increased Ei/Ai from 3.5 to 4.7, decreased Tn-I from 0.36 ng/mL to 0.18 ng/mL, decreased SVR to 3292 dynes-s-cm-5, increased DCT to 1597 msec, decreased mAoP to 66 mm Hg at 5.6 mg/kg/h.
Molecular Weight

715.86

Formula

C30H41N3O11S3

CAS No.
SMILES

CS(C1=CC=CC(OC[C@@H](O)CN[C@@H]2CC3(OC2)CCN(CC3)S(=O)(C4=CN(CC)C5=CC=CC=C5C4=O)=O)=C1)(=O)=O.CS(O)(=O)=O

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Product Name:
Vemtoberant mesylate
Cat. No.:
HY-148804A
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