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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- CAS No.: 2169905-97-7
- Formule: C30H41N3O11S3
- Masse moléculaire:715.86
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Activité biologique
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel dogs (healthy conditioned, weighing 19.9-30.6 kg, systolic heart failure model via serial intracoronary microembolizations)[1]
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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
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Administration:i.v.; continuous infusion
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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.
Chemical Information
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CAS No. 2169905-97-7
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Masse moléculaire 715.86
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Formule C30H41N3O11S3
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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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Synonyms
APD418 mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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