Doxapram HCl - 10mM in DMSO , Potassium channel subfamily K member 9 blocker, CAS No.7081-53-0, Potassium channel subfamily K member 9 blocker

CAS: 7081-53-0 Cat. No.: D408910 Molecular Weight: 432.98 EC Number: 615-173-3

GRADE & PURITY 10mM in DMSO

Synonyms

2-Pyrrolidinone, 1-ethyl-4-[2-(4-morpholinyl)ethyl]-3,3-diphenyl-, hydrochloride, hydrate (1:1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Doxapram HCl Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.
In vitro

Doxapram inhibits both TASK-1 and TASK-3 function in a dose dependent manner. Doxapram inhibition at both hyperpolarized and depolarized potentials, as well as effects independent of extracellular potassium concentration. It is said that the carboxy terminal domain of TASK-1 is important to doxapram inhibition. Doxapram also inhibits TRESK, TASK-2, and TREK-1 but at significantly larger concentrations (EC50s of 240 μM, 460 μM, and >1 mM, respectively). Doxapram has no effect on MAC for halothane.

In vivo

Doxapram is an analeptic agent. The respiratory stimulant action is manifested by an increase in tidal volume associated with a slight increase in respiratory rate. A pressor response may result following Doxapram administration.The mean half-life is 3.4 h (range 2.4-4.1h), the mean apparent volume of distribution is 1.5 mg/kg and the whole body clearance is 370 mL/min. Enteric-coated capsules of doxapram base are absorbed rapidly after an initial delay, and the systemic availability is about 60%.
Cell Data

cell lines：BT474, HCC1954 and T-47D cells

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Synonyms

2-Pyrrolidinone, 1-ethyl-4-[2-(4-morpholinyl)ethyl]-3, 3-diphenyl-, hydrochloride, hydrate (1:1:1)

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

BLOCKER

Mechanism of action

Potassium channel subfamily K member 9 blocker

Names and Identifiers

• Isomeric SMILES: CCN1CC(C(C1=O)(C2=CC=CC=C2)C3=CC=CC=C3)CCN4CCOCC4.O.Cl
• Molecular Weight: 432.98
• Reaxy-Rn: 30243666
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=30243666&ln=

References

1. Sun Kaiyue, Bai Yuting, Zhao Rong, Guo Zijiao, Su Xiang, Li Peiqi, Yang Pengyu.  (2018)  Neuroprotective effects of matrine on scopolamine-induced amnesia via inhibition of AChE/BuChE and oxidative stress.  METABOLIC BRAIN DISEASE,  34  (1): (173-181).  [PMID:30406376] [10.1007/s11011-018-0335-y]