(S)-(-)-Bay-K-8644

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Chemical Structure| 98625-26-4 同义名 : -
CAS号 : 98625-26-4
货号 : A273444
分子式 : C16H15F3N2O4
纯度 : 98%+
分子量 : 356.3
MDL号 : MFCD00153769
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 (S) -(-)-Bay K 8644 is an agonist of L-type Ca2+ channel. (S)-(-)-Bay-K-8644 activates Ba2+ currents (IBa) (EC50=32 nM). (S)-(-)-Bay-K-8644 can prevent the inhibitory actions of two distinct cyclic nucleotide pathways on IBa in gastric myocytes of the guinea pig antrum[3]. The channel activity was enhanced by 3-30 microM S(-)Bay K 8644, an agonist of L-type Ca2+ channels[4]. FPL 64176 (300 nM) causes a sustained contraction of rat tail artery strips. This contractile response is inhibited by approximately 70% by (S)-(-)-Bay-K-8644 (EC50=14 nM). (S)-Bay K 8644 (100 nM) increased whole-cell Ca2+ currents in A7r5 smooth muscle cells but effectively blocked further stimulation by 1 microM FPL 64176[5]. S-(-)-Bay K 8644 failed to produce characteristically large increases in current when cells were held at -40 mV and Ca2+ was used as the charge carrier, although high-affinity binding and the effects of the antagonist isomer, R-(+)-Bay K 8644, were intact. The pharmacology of S-(-)-Bay K 8644 in stem cell-derived cardiomyocytes varies by cell type, is unusually dependent on holding potential and charge carrier, and is different from that observed in primary human heart cells[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.07mL

5.61mL

2.81mL

参考文献

[1]Mironov SL, Richter DW. L-type Ca2+ channels in inspiratory neurones of mice and their modulation by hypoxia. J Physiol. 1998 Oct 1;512 ( Pt 1):75-87.

[2]Rampe D, Dage RC. Functional interactions between two Ca2+ channel activators, (S)-Bay K 8644 and FPL 64176, in smooth muscle. Mol Pharmacol. 1992 Apr;41(4):599-602.

[3]Zhu HL, Teramoto N. Antagonistic actions of S(-)-Bay K 8644 on cyclic nucleotide-induced inhibition of voltage-dependent Ba(2+) currents in guinea pig gastric antrum. Naunyn Schmiedebergs Arch Pharmacol. 2008 Dec;378(6):609-15

[4]Mironov SL, Richter DW. L-type Ca2+ channels in inspiratory neurones of mice and their modulation by hypoxia. J Physiol. 1998 Oct 1;512 ( Pt 1)(Pt 1):75-87

[5]Rampe D, Dage RC. Functional interactions between two Ca2+ channel activators, (S)-Bay K 8644 and FPL 64176, in smooth muscle. Mol Pharmacol. 1992 Apr;41(4):599-602

[6]Ji J, Kang J, Rampe D. L-type Ca2+ channel responses to bay k 8644 in stem cell-derived cardiomyocytes are unusually dependent on holding potential and charge carrier. Assay Drug Dev Technol. 2014 Aug;12(6):352-60