(S)-(-)-Bay-K-8644 是 L 型钙离子通道激

(S)-(-)-Bay-K-8644 is an agonist of L-type Ca²⁺ channel. (S)-(-)-Bay-K-8644 activates Ba²⁺ currents (I_Ba) (EC₅₀=32 nM).

EC50: 32 nM (I_Ba)^[1]

(±)-Bay K 8644, a conventional racemic mixture of Bay K 8644, is widely used as an L-type Ca²⁺ channel agonist. Each optical isomer possesses opposite effects on IBa (R(+)-Bay K 8644 as an antagonist and (S)-(-)-Bay-K-8644 as an agonist. (S)-(-)-Bay-K-8644 can prevent the inhibitory actions of two distinct cyclic nucleotide pathways on I_Ba in gastric myocytes of the guinea pig antrum^[1]. The Ca²⁺ channel activity is enhanced by 3–30 μM (S)-(-)-Bay-K-8644 an agonist of L-type Ca²⁺ channels^[2]. The interactions of two Ca²⁺ channel activators (S)-(-)-Bay-K-8644 and FPL 64176 is examined on smooth muscle L-type Ca²⁺channels. 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) increases whole-cell Ca²⁺ currents in A7r5 smooth muscle cells but effectively blocks further stimulation by 1 μM FPL 64176^[3].

356.30

Solid

C₁₆H₁₅F₃N₂O₄

98625-26-4

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (280.66 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 2 years; -20℃, 1 year。-80℃ 储存时，请在 2 年内使用， -20℃ 储存时，请在 1 年 内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (7.02 mM); Suspended solution; Need ultrasonic

   

  此方案可获得 2.5 mg/mL (7.02 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

• 2.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

   

  此方案可获得 ≥ 2.08 mg/mL (5.84 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

• [1]. Zhu HL, et al. 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.  [Content Brief]

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

  [3]. Rampe D, et al. 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.  [Content Brief]