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Submit ReviewFPL 64176
Description: Potent CaV1.x activator
Chemical Name: 2,5-Dimethyl-4-[2-(phenylmethyl)benzoyl]-1H-pyrrole-3-carboxylic acid methyl ester
Purity: ≥99% (HPLC)
Biological Activity for FPL 64176
FPL 64176 is a potent activator of L-type Ca2+ channels (EC50 = 16 nM). 40-fold more potent than Bay K 8644 (Cat. No. 1544) as a positive inotrope in guinea pig atria.
Technical Data for FPL 64176
| M. Wt | 347.41 |
| Formula | C22H21NO3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 120934-96-5 |
| PubChem ID | 3423 |
| InChI Key | MDMWHKZANMNXTF-UHFFFAOYSA-N |
| Smiles | COC(=O)C1=C(C)NC(C)=C1C(=O)C1=CC=CC=C1CC1=CC=CC=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FPL 64176
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 8.69 | 25 | |
| DMSO | 17.37 | 50 |
Preparing Stock Solutions for FPL 64176
The following data is based on the product molecular weight 347.41. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.76 mL | 28.78 mL | 57.57 mL |
| 2.5 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.58 mL | 2.88 mL | 5.76 mL |
| 25 mM | 0.12 mL | 0.58 mL | 1.15 mL |
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Product Datasheets for FPL 64176
References for FPL 64176
References are publications that support the biological activity of the product.
Baxter et al (1993) Discovery and synthesis of methyl 2,5-dimethyl-4-[2-(phenylmethyl)benzoyl]-1H-pyrrole-3-carboxylate (FPL 64176) and analogues: the first examples of a new class of calcium channel activator. J.Med.Chem. 36 2739 PMID: 7692047
Rampe et al (1993) Comparison of the in vitro and in vivo cardiovascular effects of two structurally distinct Ca++ channel activators, BAY K 8644 and FPL 64176. J.Pharmacol.Exp.Ther. 265 1125 PMID: 7685384
Zheng et al (1991) Pharmacological, radioligand binding, and electrophysiological characteristics of FPL 64176, a novel nondihydropyridine Ca2+ channel activator, in cardiac and vascular preparations. Mol.Pharmacol. 40 734 PMID: 1719369
If you know of a relevant reference for FPL 64176, please let us know.
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Keywords: FPL 64176, FPL 64176 supplier, Potent, activator, Ca2+, channels, L-type, Calcium, CaV, Channels, voltage-gated, voltage-dependent, FPL64176, Cav1.x, 1403, Tocris Bioscience
6 Citations for FPL 64176
Citations are publications that use Tocris products. Selected citations for FPL 64176 include:
Armstrong and Drapeau (2013) Calcium channel agonists protect against neuromuscular dysfunction in a genetic model of TDP-43 mutation in ALS. Circ Heart Fail 33 1741 PMID: 23345247
Landstrom et al (2011) Junctophilin-2 expression silencing causes cardiocyte hypertrophy and abnormal intracellular calcium-handling. Endocr Relat Cancer 4 214 PMID: 21216834
Zhang et al (2011) AKAP79/150 signal complexes in G-protein modulation of neuronal ion channels. J Neurosci 31 7199 PMID: 21562284
Zhong (2018) Intracellular emetic signaling evoked by the L-type Ca2+ channel agonist FPL64176 in the least shrew (Cryptotis parva). Eur J Pharmacol 834 157 PMID: 29966616
Large et al (2010) Ionic currents in intimal cultured synoviocytes from the rabbit. Am J Physiol Cell Physiol 299 C1180 PMID: 20720182
Won et al (2012) Characterization of Na+ and Ca2+ channels in zebrafish dorsal root ganglion neurons. PLoS One 7 e42602 PMID: 22880050
Do you know of a great paper that uses FPL 64176 from Tocris? Please let us know.
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