NP118809N-type calcium channel blocker CAS# 41332-24-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 41332-24-5 | SDF | Download SDF |
| PubChem ID | 4988454 | Appearance | Powder |
| Formula | C32H32N2O | M.Wt | 460.61 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 50 mg/mL (108.55 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one | ||
| SMILES | C1CN(CCN1C(C2=CC=CC=C2)C3=CC=CC=C3)C(=O)CC(C4=CC=CC=C4)C5=CC=CC=C5 | ||
| Standard InChIKey | VCPMZDWBEWTGNW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C32H32N2O/c35-31(25-30(26-13-5-1-6-14-26)27-15-7-2-8-16-27)33-21-23-34(24-22-33)32(28-17-9-3-10-18-28)29-19-11-4-12-20-29/h1-20,30,32H,21-25H2 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
NP118809 Dilution Calculator
NP118809 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.171 mL | 10.8552 mL | 21.7103 mL | 43.4207 mL | 54.2759 mL |
| 5 mM | 0.4342 mL | 2.171 mL | 4.3421 mL | 8.6841 mL | 10.8552 mL |
| 10 mM | 0.2171 mL | 1.0855 mL | 2.171 mL | 4.3421 mL | 5.4276 mL |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 0.8684 mL | 1.0855 mL |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.4342 mL | 0.5428 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Description: IC50 Value: 0.11uM (for N-type Calcium channel) [1] NP-118809 is a potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. in vitro: NP-118809, exhibited increased N-type channel blockade (IC50=0.11 uM) and was 111-fold more selective for N-type channels (L-type calcium channel IC50=12.2 uM) [1]. In the N,4-dibenzhydryl-piperazine-1-carboxamide series (21-27), non-substituted derivative (21) showed a similar inhibitory activity for N-type calcium channels (est. IC50=0.15 uM) as that of parent compound, NP-118809 (est. IC50=0.11 uM). 1-[Phenyl(pyridin-4-yl)methyl]piperazine (42), with no substituent on the nitrogen showed good N-type blocking activity (est. IC50=0.06 uM) while the N-methylated analog (43) was an order of magnitude less potent (est. IC50=0.69 uM) [2]. in vivo: NP-118809, i.v. at 2 mg/kg or p.o. at 10 mg/kg in rats, showed acceptable absorption (Tmax=2.3 hr) and half-life (2.1 hr) characteristics and a mean oral bioavailability of 30%. Both compounds were widely distributed outside of plasma and/or bound to plasma proteins. Upon i.p. administration of NP-118809 and NP-078585 at 25 mg/kg, both showed analgesic activity in Phase IIA portions of the rat formalin model. A single 1 uM dose application of NP-078585 blocked hERG currents showing its potential for cardiovascular liability [1]. Clinical trial:
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Scaffold-based design and synthesis of potent N-type calcium channel blockers.[Pubmed:19815411]
Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72.
The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optimization, we discovered NP118809 and NP078585, two potent N-type calcium channel blockers which have good selectivity over L-type calcium channels. Upon intraperitoneal administration both compounds exhibit analgesic activity in a rodent model of inflammatory pain. NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.[Pubmed:20117000]
Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83.
A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC(50) values in the range of 10-150 nM and selectivity over the L-type channels up to nearly 1200-fold. Orally administered compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain.
