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Submit Review(R)-(+)-Bay K 8644 is a L-type Ca2+-channel blocker with negative inotropic and vasodilatatory effects in vivo. Enantiomer showing opposite effects to the racemate (±)-Bay K 8644 (Cat. No. 1544) and (S)-(-)- enantiomer (Cat. No. 1546). Also TMEM176B inhibitor. Induces IL-1β secretion and caspase-1 activation in bone marrow-derived dendritic cells in vitro and increases survival of tumor-bearing mice, both alone and in combination with immune checkpoint blockers.
Racemate and (S)-(-)-Enantiomer also available.
(R)-(+)-Bay K 8644 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 356.3 |
公式 | C16H15F3N2O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 98791-67-4 |
PubChem ID | 6604881 |
InChI Key | ZFLWDHHVRRZMEI-CYBMUJFWSA-N |
Smiles | O=C(OC)C1=C(C)NC(C)=C([N+]([O-])=O)[C@@H]1[C@]2=CC=CC=C2C(F)(F)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 35.63 | 100 | |
DMSO | 35.63 | 100 |
以下数据基于产品分子量 356.3。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.81 mL | 14.03 mL | 28.07 mL |
5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
10 mM | 0.28 mL | 1.4 mL | 2.81 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
参考文献是支持产品生物活性的出版物。
Franckowiak et al (1985) The optical isomers of the 1,4-dihydropyridine BAY K 8644 show opposite effects on Ca channels. Eur.J.Pharmacol. 114 223 PMID: 2412855
O'Neill and Bolger (1988) Enantiomer selectivity and the development of tolerance to the behavioral effects of the calcium channel activator BAY K 8644. Brain Res.Bull. 21 865 PMID: 2465070
Ravens and Schopper (1990) Opposite cardiac actions of the enantiomers of Bay K 8644 at different membrane potentials in guinea-pig papillary muscles. Naunyn Schmiedebergs Arch.Pharmacol. 341 232 PMID: 1692975
Shi et al (2008) Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds. Cell Stem Cell. 3 568 PMID: 18983970
Segovia et al (2019) Targeting TMEM176B enhances antitumor immunity and augments the efficacy of immune checkpoint blockers by unleashing inflammasome activation. Cancer Cell. 35 767 PMID: 31085177
If you know of a relevant reference for (R)-(+)-Bay K 8644, please let us know.
关键词: (R)-(+)-Bay K 8644, (R)-(+)-Bay K 8644 supplier, Ca2+-channel, blockers, L-type, Calcium, CaV, Channels, L-Type, voltage-gated, voltage-dependent, Ca2+, (R)-(+)-BayK8644, stem, cells, TMEM176B, transmembrane, protein, immune, checkpoint, inhibitors, inhibits, activates, inflammasomes, Cav1.x, Immune, Checkpoints, Inflammasomes, Other, Channel, Modulators, 1545, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (R)-(+)-Bay K 8644 的部分引用包括:
Sidaway and Teramoto (2014) L-type Ca2+ channel sparklets revealed by TIRF microscopy in mouse urinary bladder smooth muscle. PLoS One 9 e93803 PMID: 24699670
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R-(+)-Bay-K (5 μM) was used as a part of a mixture (also containing 1 μM omega -Conotoxin GVIA and 1 μM omega -Agatoxin TK) which blocks voltage-gated calcium channels in a living neuron membrane. Left: the effect of activation of 5HT-1B and AMPA receptors on transmembrane current evoked upon membrane depolarization. Blue trace: control; red trace: 5HT-1B and AMPA receptors activation. Right: block of VGCCs results in 100% suppression of transmembrane current.