Cat. No.: HY-17457

Levalbuterol hemitartrate

(Synonyms: Levosalbutamol hemitartrate)

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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.

Purity: 98.71%
CAS No.: 661464-94-4
Formula: C₁₃H₂₁NO₃·1/2C₂H₆O₆
Molecular Weight:314.37

Storage:

4°C, sealed storage, away from moisture

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

Levalbuterol hemitartrate Chemical Structure

CAS No.: 661464-94-4

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

β adrenergic receptor

PI3K

All Adrenergic Receptor Isoforms :

All PI3K Isoforms :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 661464-94-4
Appearance Solid
Molecular Weight 314.37
Formula C₁₃H₂₁NO₃·1/2C₂H₆O₆
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]
Synonyms

Levosalbutamol hemitartrate
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1810 mL

15.9048 mL

31.8097 mL

5 mM

0.6362 mL

3.1810 mL

6.3619 mL

10 mM

0.3181 mL

1.5905 mL

3.1810 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ibe BO, et al. Levalbuterol inhibits human airway smooth muscle cell proliferation: therapeutic implications in the management of asthma. Int Arch Allergy Immunol. 2006;139(3):225-236. [Content Brief]

[2]. Nelson HS, et al. Improved bronchodilation with levalbuterol compared with racemic albuterol in patients with asthma. J Allergy Clin Immunol. 1998;102(6 Pt 1):943-952. [Content Brief]

[3]. Ameredes BT, Calhoun WJ. Levalbuterol versus albuterol. Curr Allergy Asthma Rep. 2009 Sep;9(5):401-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Levalbuterol hemitartrate

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All Adrenergic Receptor Isoforms

All PI3K Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Levalbuterol hemitartrate Related Classifications

HY-17457 Related Classifications