D7443
DPO-1
needles, >97% (NMR)
别名:
(+)-Neomenthyl diphenylphosphine oxide, (1S,2S,5R)-5-Methyl-2-(1-methylethyl)cyclohexyl]diphenyl-phosphine oxide
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选择尺寸
关于此项目
经验公式（希尔记法）:
C22H29OP
化学文摘社编号:
分子量:
340.44
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C22H29OP/c1-17(2)21-15-14-18(3)16-22(21)24(23,19-10-6-4-7-11-19)20-12-8-5-9-13-20/h4-13,17-18,21-22H,14-16H2,1-3H3/t18-,21+,22+/m1/s1
SMILES string
CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1P(=O)(c2ccccc2)c3ccccc3
InChI key
BPCNGVCAHAIZEE-COPCDDAFSA-N
assay
>97% (NMR)
form
needles
storage condition
protect from light
color
white
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Biochem/physiol Actions
DPO-1 is an inhibitor of human Kv1.5 potassium channel; representative blocker of a novel pharmacophore.
DPO-1 is an inhibitor of human Kv1.5 potassium channel; representative blocker of a novel pharmacophore. The Kv1.5 potassium channel, which underlies the ultrarapid delayed rectifier current, IKur, is reported to be enriched in human atrium versus ventricle, and has been proposed as a target for novel atrial antiarrhythmic therapy. The administration of the IKur blocker (2-isopropyl-5-methyl-cyclohexyl) diphenylphosphine oxide (DPO-1) increases myocardial refractoriness in both atrium and ventricle of rat, but produces an atrial-selective increase in refractoriness in primates; appears to be 15-fold more selective for Kv1.5 vs Kv3.1 channels expressed in Xenopus oocytes. IC50 = 0.16-0.76 μM at 0.1 Hz pulsing frequency; Kd = 0.6 μM.
Features and Benefits
This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Anastasia A Shvetsova et al.
British journal of pharmacology, 177(22), 5148-5162 (2020-08-30)
The vasomotor role of K2P potassium channels during early postnatal development has never been investigated. We tested the hypothesis that TASK-1 channel (K2P family member) contribution to arterial vascular tone and BP is higher in the early postnatal period than
Hongliang Li et al.
European journal of pharmacology, 849, 59-66 (2019-02-05)
In the present study, we investigated the inhibitory effect of tacrolimus, a macrolide immunosuppressive drug that acts through calcineurin inhibition, on voltage-gated K+ (Kv) channels expressed in native smooth muscle cells isolated from the coronary arteries of rabbits. Tacrolimus reduced
Ning Zhao et al.
PloS one, 8(5), e64629-e64629 (2013-05-30)
Diphenyl phosphine oxide-1 (DPO-1) is a potent Kv1.5 channel inhibitor that has therapeutic potential for the treatment of atrial fibrillation. Many other Kv1.5 channel blockers also potently inhibit the Kv1.3 channel, but whether DPO-1 blocks Kv1.3 channels has not been
Olga Zavaritskaya et al.
British journal of pharmacology, 177(5), 1164-1186 (2019-10-29)
BK channels play important roles in various physiological and pathophysiological processes and thus have been the target of several drug development programmes focused on creating new efficacious BK channel openers, such as the GoSlo-SR compounds. However, the effect of GoSlo-SR
Han Sol Kim et al.
The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology, 21(4), 415-421 (2017-07-15)
We investigated the inhibitory effect of escitalopram, a selective serotonin reuptake inhibitor (SSRI), on voltage-dependent K
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