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About This Item
実験式（ヒル表記法）:
C28H38N2O5 · HCl
CAS番号:
分子量:
519.07
MDL番号:
UNSPSCコード:
12352200
PubChem Substance ID:
NACRES:
NA.77
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品質水準
アッセイ
≥98% (HPLC)
フォーム
solid
色
white
溶解性
H2O: ~20 mg/mL
保管温度
2-8°C
SMILES記法
O=C1CC2=CC(OC)=C(OC)C=C2CCN1C[C@@H](CCC3)CN3CCC4=CC(OC)=C(OC)C=C4.[H]Cl
InChI
1S/C28H38N2O5.ClH/c1-32-24-8-7-20(14-25(24)33-2)9-12-29-11-5-6-21(18-29)19-30-13-10-22-15-26(34-3)27(35-4)16-23(22)17-28(30)31;/h7-8,14-16,21H,5-6,9-13,17-19H2,1-4H3;1H/t21-;/m0./s1
InChI Key
MTAKUIYCCYKGJJ-BOXHHOBZSA-N
アプリケーション
DK-AH 269 has been used as a hyperpolarization-activated and cyclic nucleotide-gated channel (HCN) antagonist to study its effects on the inhibition of Ih in HCN-deficient hair cells of mice. It has also been used as an HCN blocker to study its effects on action potential firing in the suprachiasmatic nucleus (SCN) neurons.
生物化学的／生理学的作用
DK-AH 269 (Cilobradine) is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.
DK-AH 269 is a bradycardiac agent.
特徴および利点
This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Cyclic Nucleotide-Gated (CNG) and Hyperpolarization Activated Cyclic Nucleotide-Gated (HCN) Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
個人用保護具 (PPE)
Eyeshields, Gloves, type N95 (US)
最新バージョンのいずれかを選択してください：
HCN channels expressed in the inner ear are necessary for normal balance function
Horwitz G C, et al.
The Journal of Neuroscience, 31(46), 16814-16825 (2011)
A Raes et al.
British journal of pharmacology, 125(4), 741-750 (1998-12-01)
1. The sinus node inhibitors UL FS 49 and DK-AH 269 reduce heart rate by slowing diastolic depolarization rate in the sino-atrial (SA) node, which might originate from the use-dependent blockade of a hyperpolarization-activated current If. A hyperpolarization-activated current Ih
Vivien Chevaleyre et al.
Proceedings of the National Academy of Sciences of the United States of America, 99(14), 9538-9543 (2002-07-03)
Hyperpolarization-activated nonselective cation channels (Ih channels) play an important role in the control of membrane excitability and rhythmic neuronal activity. The functional relevance of presynaptic Ih channels in regulating synaptic function, however, is not well established. Recently, it has been
Effects of a bradycardic agent (DK-AH 269) on haemodynamics and oxygen consumption of isolated blood-perfused rabbit hearts
Granetzny A, et al.
Journal of Clinical and Basic Cardiology, 3(3), 191-196 (2000)
Specific bradycardic agents block the hyperpolarization-activated cation current in central neurons.
H C Pape
Neuroscience, 59(2), 363-373 (1994-03-01)
A class of pharmacologically active substances, known as "specific bradycardic agents", exerts a negative chronotropic influence on cardiac activity, which heavily relies upon a potent blockade of the hyperpolarization-activated cation current in Purkinje fibers. Since the cation conductance activated by
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