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.
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- CAS No.: 99453-84-6
- 화학식: C18H20Br2N2O2S
- 분자량:488.24
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보관:
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
- 순도&문서
- 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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분자량 488.24
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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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