1. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR
  2. Adrenergic Receptor PI3K
  3. Levalbuterol hemitartrate

Levalbuterol hemitartrate  (Synonyms: Levosalbutamol hemitartrate)

Cat. No.: HY-17457 Purity: 98.71%
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Levalbuterol (Levosalbutamol) hemitartrate is a β2-adrenergic receptor agonist and PI3K inhibitor. Levalbuterol hemitartrate inhibits PI3K activity, reduces NF-κB and Rb protein expression, activates the cAMP/PKA pathway, and stimulates cAMP release. Levalbuterol hemitartrate relaxes airway smooth muscle, reduces intracellular calcium levels, and inhibits spasmogen-induced contractions. Levalbuterol hemitartrate can be used for the research of moderate-to-severe asthma.

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

Levalbuterol hemitartrate

Levalbuterol hemitartrate Chemical Structure

CAS No. : 661464-94-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

Levalbuterol (Levosalbutamol) hemitartrate is a β2-adrenergic receptor agonist and PI3K inhibitor. Levalbuterol hemitartrate inhibits PI3K activity, reduces NF-κB and Rb protein expression, activates the cAMP/PKA pathway, and stimulates cAMP release. Levalbuterol hemitartrate relaxes airway smooth muscle, reduces intracellular calcium levels, and inhibits spasmogen-induced contractions. Levalbuterol hemitartrate can be used for the research of moderate-to-severe asthma[1][2][3].

IC50 & Target[1]

β adrenergic receptor

 

PI3K

 

In Vitro

Levalbuterol (0.001-100 μM; 24 h) inhibits human bronchial smooth muscle cell proliferation in a biphasic manner, with maximum 80% inhibition at 0.1 μM, via β2-adrenergic receptor and cAMP/PKA pathway activation[1].
Levalbuterol (1 μM; 24 h) hemitartrate has an inhibitory effect on human bronchial smooth muscle cell proliferation that is completely abrogated by preincubation with 1 μM β2-adrenergic receptor antagonist ICI-118551 (HY-100543) (2 h preincubation)[1].
Levalbuterol (1 μM; 2 h) hemitartrate has an inhibitory effect on human bronchial smooth muscle cell proliferation that is attenuated or abrogated, respectively, by co-treatment with 1 μM or 10 μM (S)-Albuterol (HY-137311A) (24 h)[1].
Levalbuterol (1 μM; 24 h) hemitartrate has an inhibitory effect on human bronchial smooth muscle cell proliferation that is enhanced by co-treatment with 10 μM 8-Br-cAMP (HY-12306A) (2 h preincubation) and completely abrogated by co-treatment with 10 μM Rp-cAMPS (HY-100530A) (2 h preincubation), confirming involvement of the cAMP/PKA pathway[1].
Levalbuterol (0.1-1.0 μM; 15 min) hemitartrate stimulates cAMP release in human bronchial smooth muscle cells, an effect that is attenuated by 65% with co-treatment of 1.0 μM (S)-Albuterol (15 min)[1].
Levalbuterol (1.0 μM; 20 min) hemitartrate inhibits inositol phosphate release by 50% in human bronchial smooth muscle cells, indicating inhibition of PI-3 kinase activity[1].
Levalbuterol (1.0 μM; 24 h) hemitartrate inhibits NF-κB protein expression by 50% and Rb protein expression by 40% in human bronchial smooth muscle cells[1].
Levalbuterol hemitartrate induces airway smooth muscle relaxation and reduces spasmogen-induced contractions in in vitro ASM cells/tissues from horse, cow, guinea pig, mouse, and human sources via β2-adrenoreceptor ligation-dependent mechanisms[3].
Levalbuterol hemitartrate exerts anti-inflammatory effects in human eosinophils and T lymphocytes by inhibiting proinflammatory mediator release and T-cell proliferation via β2-adrenoreceptor ligation[3].
Levalbuterol hemitartrate reduces proinflammatory GM-CSF release from human ASM cells, enhances corticosteroid-mediated suppression of cytokine release, and modulates intracellular cAMP and NF-κB signaling pathways via β2-adrenoreceptors[3].

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

Cell Proliferation Assay[1]

Cell Line: human bronchial smooth muscle cells (HBSMCs)
Concentration: 0.001 μM; 0.01 μM; 0.1 μM; 10 μM; 100 μM
Incubation Time: 24 h
Result: Showed a biphasic inhibitory effect on HBSMC proliferation.
Produced 5% inhibition relative to 5% FBS control at 0.001 μM.
Increased inhibition to 40% at 0.01 μM.
Reached a maximum of 80% inhibition at 0.1 μM.
Decreased inhibition to 55% at 1.0 μM.
Further decreased inhibition at 10 μM.
Showed no inhibitory effect at 100 μM.
Maintained cell viability >95% across all doses.

Cell Proliferation Assay[1]

Cell Line: human bronchial smooth muscle cells (HBSMCs)
Concentration: 1 μM; 1 μM plus 1 μM ICI-118551
Incubation Time: 24 h
Result: Produced 57% inhibition of HBSMC proliferation relative to 5% FBS control with 1 μM levalbuterol alone.
Completely abrogated this inhibitory effect when co-incubated with 1 μM ICI-118551, restoring cell proliferation to the 5% FBS control level.

Cell Proliferation Assay[1]

Cell Line: human bronchial smooth muscle cells (HBSMCs)
Concentration: 1 μM; 1 μM plus 1 μM (S)-Albuterol; 1 μM plus 10 μM (S)-Albuterol)
Incubation Time: 2 h
Result: Produced 80% inhibition of HBSMC proliferation relative to 5% FBS control with 1 μM levalbuterol alone.
Reduced this inhibition to 20% when co-treated with 1 μM (S)-Albuterol.
Completely abrogated the inhibitory effect of levalbuterol when co-treated with 10 μM (S)-Albuterol.

Cell Proliferation Assay[1]

Cell Line: human bronchial smooth muscle cells (HBSMCs)
Concentration: 1 μM; 1 μM plus 10 μM 8-Br-cAMP; 1 μM plus 10 μM Rp-cAMPS
Incubation Time: 24 h
Result: Produced 65% inhibition of HBSMC proliferation with 10 μM 8-Br-cAMP alone.
Resulted in an additive inhibitory effect (75% total inhibition) when co-treated with 1 μM levalbuterol.
Increased proliferation by 30% relative to 5% FBS with 10 μM Rp-cAMPS alone.
Caused a 2-fold increase in proliferation and completely abrogated levalbuterol's inhibitory effect when co-treated with 1 μM levalbuterol.

Cell Proliferation Assay[1]

Cell Line: human bronchial smooth muscle cells (HBSMCs)
Concentration: 1 μM (levalbuterol); 30 μM (LY294002, preincubation); 30 μM (wortmannin, preincubation)
Incubation Time: 24 h
Result: Produced 90% inhibition of HBSMC proliferation with 30 μM LY294002 alone.
Produced 85% inhibition of HBSMC proliferation with 30 μM wortmannin alone.
Did not restore proliferation to levels seen with levalbuterol alone when co-treated with 1 μM levalbuterol.

Western Blot Analysis[1]

Cell Line: human bronchial smooth muscle cells (HBSMCs)
Concentration: 1.0 μM
Incubation Time: 24 h
Result: Caused a 50% decrease in NF-κB protein expression relative to 5% FBS control.
Caused a 40% decrease in Rb protein expression relative to 5% FBS control.
Clinical Trial
Molecular Weight

314.37

Formula

C13H21NO3·1/2C2H6O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC([C@H](O)[C@@H](O)C(O)=O)=O.CC(C)(C)NC[C@@H](C1=CC(CO)=C(C=C1)O)O.[1/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (318.10 mM; Need ultrasonic)

DMSO : 17.5 mg/mL (55.67 mM; ultrasonic and warming and heat to 60°C; 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 3.1810 mL 15.9048 mL 31.8097 mL
5 mM 0.6362 mL 3.1810 mL 6.3619 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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 (sealed storage, away from moisture). 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 / H2O 1 mM 3.1810 mL 15.9048 mL 31.8097 mL 79.5241 mL
5 mM 0.6362 mL 3.1810 mL 6.3619 mL 15.9048 mL
10 mM 0.3181 mL 1.5905 mL 3.1810 mL 7.9524 mL
15 mM 0.2121 mL 1.0603 mL 2.1206 mL 5.3016 mL
20 mM 0.1590 mL 0.7952 mL 1.5905 mL 3.9762 mL
25 mM 0.1272 mL 0.6362 mL 1.2724 mL 3.1810 mL
30 mM 0.1060 mL 0.5302 mL 1.0603 mL 2.6508 mL
40 mM 0.0795 mL 0.3976 mL 0.7952 mL 1.9881 mL
50 mM 0.0636 mL 0.3181 mL 0.6362 mL 1.5905 mL
H2O 60 mM 0.0530 mL 0.2651 mL 0.5302 mL 1.3254 mL
80 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
100 mM 0.0318 mL 0.1590 mL 0.3181 mL 0.7952 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    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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