Neltenexine
Neltenexine is a mucolytic agent and an inhibitor of anion hypersecretion. Neltenexine acts on NKCC1, NBC1 and AE2 transporters located on the basolateral membrane of airway epithelial cells. Neltenexine reduces Cl-/HCO3- uptake by inhibiting NKCC1 and NBC1, activates AE2 to promote Cl- excretion, reduces β2-adrenergic agonist-induced anion hypersecretion without blocking CFTR channels, and maintains appropriate airway fluid levels. Neltenexine can be used in research related to chronic obstructive pulmonary disease and emphysema.
For research use only. We do not sell to patients.
- CAS No.: 99453-84-6
- Formula: C18H20Br2N2O2S
- Molecular Weight:488.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Neltenexine (100 μM) reduces Terbutaline (HY-B0802A)-stimulated anion (Cl- and HCO3-) secretion in Calu-3 cells by inhibiting basolateral anion uptake transporters, without altering Na+ absorption[1].
Neltenexine (100 μM) reduces Terbutaline-stimulated Cl- secretion in Calu-3 cells under HCO3--free conditions. Its mechanism of action involves inhibiting the activity of the basolateral Na+/K+/2Cl- cotransporter (NKCC1) without altering Na+ absorption[1].
Neltenexine (100 μM) reduces terbutaline-stimulated anion secretion in bumetanide (HY-17468)-pretreated Calu-3 cells by inhibiting basolateral NBC1 activity and activating the Cl-/HCO3- exchanger (AE2)[1].
Neltenexine (100 μM) reduces Terbutaline-stimulated HCO3- secretion in Cl--free Calu-3 cells by inhibiting basolateral NBC1 activity[1].
Neltenexine (100 μM) exerts no net effect on basal anion (Cl- and HCO3-) secretion in Calu-3 cells under in vitro conditions with the simultaneous presence of Cl- and HCO3-[1].
Neltenexine (100 μM) reduces basal Cl- secretion in Calu-3 cells under HCO3- -free conditions by inhibiting the activity of basolateral NKCC1[1].
Neltenexine (100 μM) reduces basal HCO3- secretion in Cl--free Calu-3 cells by inhibiting the activity of basolateral NBC1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 99453-84-6
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Molecular Weight 488.24
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Formula C18H20Br2N2O2S
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SMILES
O=C(C1=CC=CS1)NC2=C(C=C(C=C2Br)Br)CN[C@H]3CC[C@@H](CC3)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Niisato N, et al. Action of neltenexine on anion secretion in human airway epithelia. Biochemical and biophysical research communications. 2007 May 18;356(4):1050-5. [Content Brief]
[2]. Braga PC, et al. Neltenexine: morphological investigation of protection against elastase-induced emphysema in rats. Drugs under experimental and clinical research. 1995;21(2):51-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Neltenexine Related Classifications
HY-165407 Related Classifications
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