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

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

For research use only. We do not sell to patients.

Vemtoberant

Vemtoberant Chemical Structure

CAS No. : 2169905-68-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Vemtoberant Related Antibodies

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Description

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

In Vivo

Vemtoberant (APD418) (0.35-15.0 mg/kg/h; i.v.; continuous infusion; 30 minutes, 60 minutes, 6 hours) 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 (total 4.224 mg/kg); 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; 30 minutes; 60 minutes; 6 hours
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

619.75

Formula

C29H37N3O8S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (403.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6136 mL 8.0678 mL 16.1355 mL
5 mM 0.3227 mL 1.6136 mL 3.2271 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6136 mL 8.0678 mL 16.1355 mL 40.3388 mL
5 mM 0.3227 mL 1.6136 mL 3.2271 mL 8.0678 mL
10 mM 0.1614 mL 0.8068 mL 1.6136 mL 4.0339 mL
15 mM 0.1076 mL 0.5379 mL 1.0757 mL 2.6893 mL
20 mM 0.0807 mL 0.4034 mL 0.8068 mL 2.0169 mL
25 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6136 mL
30 mM 0.0538 mL 0.2689 mL 0.5379 mL 1.3446 mL
40 mM 0.0403 mL 0.2017 mL 0.4034 mL 1.0085 mL
50 mM 0.0323 mL 0.1614 mL 0.3227 mL 0.8068 mL
60 mM 0.0269 mL 0.1345 mL 0.2689 mL 0.6723 mL
80 mM 0.0202 mL 0.1008 mL 0.2017 mL 0.5042 mL
100 mM 0.0161 mL 0.0807 mL 0.1614 mL 0.4034 mL
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Vemtoberant Related Classifications

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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.

Keywords:

Vemtoberant2169905-68-2APD418APD 418APD-418Adrenergic ReceptorBeta Receptorleft ventricular diastolic functionleft ventricular systolic functiondogssystolic heart failureβ1-ARcanine β3-ARβ2-ARβ3-adrenergic receptorcardiodepressionInhibitorinhibitorinhibit

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