EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72362_C
L型钙通道抑制剂
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总览
(+)-Bay K8644 是一种潜在调控钙通道的调节剂，存在两种作用相反的对映体 (Hess et al.; Nowycky et al.; O'Neill et al.; Ravens et al.; Yamamoto et al.)。(+)-Bay K8644 是一种 L 型通道阻滞剂，具有负性肌力和血管扩张作用 (Artigas et al.; Franckowiak et al.; Ravens et al.)。
重编程
·当与BIX-01294联合使用时，仅用OCT4和KLF4转导后即可实现小鼠胚胎成纤维细胞的重编程（Shi et al.）。
分化
·促进小鼠出生后脑神经干细胞和祖细胞 (NSC) 向神经元的分化（D'Ascenzo et al.）。
别名
(+)-Bay-K 8644；(+)-Bay-R 4407；(R)-(+)-Bay K 8644；NI 105；R 4407
细胞类型
神经干/祖细胞，神经元，多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
分化，重编程
CAS 编号
98791-67-4
化学式
C₁₆H₁₅F₃N₂O₄
分子量
356.3 g/mol
纯度
≥ 95 %
通路
L型钙通道
靶点
L型钙通道
产品说明书及文档
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应用领域
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相关材料与文献
技术资料 (3)
文献 (9)
Effects of the enantiomers of BayK 8644 on the charge movement of L-type Ca channels in guinea-pig ventricular myocytes.
The Journal of membrane biology 2003 JUN
Abstract
The effects of the agonist enantiomer S(-)Bay K 8644 on gating charge of L-type Ca channels were studied in single ventricular myocytes. From a holding potential (Vh) of -40 mV,saturating (250 nm) S(-)Bay K shifted the half-distribution voltage of the activation charge (Q1) vs. V curve -7.5 +/- 0.8 mV,almost identical to the shift produced in the Ba conductance vs. V curve (-7.7 +/- 2 mV). The maximum Q1 was reduced by 1.7 +/- 0.2 nC/microF,whereas Q2 (charge moved in inactivated channels) was increased in a similar amount (1.4 +/- 0.4 nC/microF). The steady-state availability curves for Q1,Q2,and Ba current showed almost identical negative shifts of -14.8 +/- 1.7 mV,-18.6 +/- 5.8 mV,and -15.2 +/- 2.7 mV,respectively. The effects of the antagonist enantiomer R(+)BayK 8644 were also studied,the Q1 vs. V curve was not significantly shifted,but Q1max (Vh = -40 mV) was reduced and the Q1 availability curve shifted by -24.6 +/- 1.2 mV. We concluded that: a) the left shift in the Q1 vs. V activation curve produced by S(-)BayK is a purely agonistic effect; b) S(-)BayK induced a significantly larger negative shift in the availability curve than in the Q1 vs. V relation,consistent with a direct promotion of inactivation; c) as expected for a more potent antagonist,R(+)Bay K induced a significantly larger negative shift in the availability curve than did S(-)Bay K.
Role of L-type Ca2+ channels in neural stem/progenitor cell differentiation.
The European journal of neuroscience 2006 FEB
Abstract
Ca(2+) influx through voltage-gated Ca(2+) channels,especially the L-type (Ca(v)1),activates downstream signaling to the nucleus that affects gene expression and,consequently,cell fate. We hypothesized that these Ca(2+) signals may also influence the neuronal differentiation of neural stem/progenitor cells (NSCs) derived from the brain cortex of postnatal mice. We first studied Ca(2+) transients induced by membrane depolarization in Fluo 4-AM-loaded NSCs using confocal microscopy. Undifferentiated cells (nestin(+)) exhibited no detectable Ca(2+) signals whereas,during 12 days of fetal bovine serum-induced differentiation,neurons (beta-III-tubulin(+)/MAP2(+)) displayed time-dependent increases in intracellular Ca(2+) transients,with DeltaF/F ratios ranging from 0.4 on day 3 to 3.3 on day 12. Patch-clamp experiments revealed similar correlation between NSC differentiation and macroscopic Ba(2+) current density. These currents were markedly reduced (-77%) by Ca(v)1 channel blockade with 5 microm nifedipine. To determine the influence of Ca(v)1-mediated Ca(2+) influx on NSC differentiation,cells were cultured in differentiative medium with either nifedipine (5 microm) or the L-channel activator Bay K 8644 (10 microm). The latter treatment significantly increased the percentage of beta-III-tubulin(+)/MAP2(+) cells whereas nifedipine produced opposite effects. Pretreatment with nifedipine also inhibited the functional maturation of neurons,which responded to membrane depolarization with weak Ca(2+) signals. Conversely,Bay K 8644 pretreatment significantly enhanced the percentage of responsive cells and the amplitudes of Ca(2+) transients. These data suggest that NSC differentiation is strongly correlated with the expression of voltage-gated Ca(2+) channels,especially the Ca(v)1,and that Ca(2+) influx through these channels plays a key role in promoting neuronal differentiation.
Opposite cardiac actions of the enantiomers of Bay K 8644 at different membrane potentials in guinea-pig papillary muscles.
Naunyn-Schmiedeberg's archives of pharmacology 1990 MAR
Abstract
The influence of membrane potential on the effects of the enantiomers and the racemate of Bay K 8644 [1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluor-methylphenyl)-p yri dine-5-carboxylate] on force of contraction and on action potentials were studied in guinea-pig papillary muscles in order to detect possible changes in the direction of drug action or in potency. Membrane potential was varied by changing the potassium concentration ([K+]o) in the bathing solution. At normal resting potential,(-)-Bay K 8644 enhanced force of contraction and prolonged the action potential duration measured at 50% of repolarization (APD) to the same extent as the racemate and with similar pD2 values. After membrane depolarization by raising [K+]o from 5.4 to 17.4 mmol/l,the (-)-enantiomer and the racemate prolonged the APD to a similar degree but enhanced force to a lesser extent. The maximum rate of depolarization of slow action potentials,Vmax,was increased at the highest concentrations (10(-5) mol/l). The effects of (+)-Bay K 8644 were more complicated. At high concentrations (10(-5) mol/l) it decreased force of contraction and APD,the pD2 values were one order of magnitude lower than for the (-)-enantiomer and the racemate. A high concentration (+)-Bay K 8644 (10(-5) mol/l) virtually abolished contractile activity at all membrane potentials,the extent of shortening in APD increased with membrane depolarization in elevated [K+]o. Vmax of slow action potentials was decreased.(ABSTRACT TRUNCATED AT 250 WORDS)
更多信息
| Molecular Weight | 356.3 g/mol |
|---|---|
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
| Alternative Names | (+)-Bay-K 8644; (+)-Bay-R 4407; (R)-(+)-Bay K 8644; NI 105; R 4407 |
| Cas Number | 98791-67-4 |
| Chemical Formula | C₁₆H₁₅F₃N₂O₄ |
| 纯度 | ≥ 95 % |
| Target | L-type Calcium Channel |
| Pathway | L-type Calcium Channel |
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产品仅供研究使用，不用于针对人或动物的诊断或治疗。
产品仅供研究使用，不用于针对人或动物的诊断或治疗。
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