| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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NP-118809 is a N-type calcium channel blocker. NP-118809 exhibits both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic 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.
| ln Vitro |
NP118809 has a strong inhibitory effect on N-type calcium channels, having an IC50 of 0.11 μM, and an IC50 of 12.2 μM on L-type calcium channels. In HEK cells, NP118809 blocks hERG potassium channels with an IC50 of 7.4 μM[1].
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| ln Vivo |
The rat formalin model's phase IIA section demonstrated notable analgesic action in response to NP118809 (25 mg/kg, i.p.) [1]. NP118809 (30 mg/kg, orally) reduced 96.3% of thermal hyperalgesia and 80.3% of mechanical allodynia in a rat spinal nerve ligation model [2].
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| References | |
| Additional Infomation |
Z160 has been used in trials studying the treatment of Postherpetic Neuralgia and Lumbosacral Radiculopathy.
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| Molecular Formula |
C32H32N2O
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|---|---|
| Molecular Weight |
460.621
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| Exact Mass |
460.251
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| CAS # |
41332-24-5
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| Related CAS # |
41332-24-5
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| PubChem CID |
4988454
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
618.9±55.0 °C at 760 mmHg
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| Flash Point |
251.4±23.9 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.622
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| LogP |
6.51
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
582
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VCPMZDWBEWTGNW-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one
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| Synonyms |
39-1B4 NP 118809 NP-118809 NP118809 Z160 Z160 Z160.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~108.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.43 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1710 mL | 10.8549 mL | 21.7099 mL | |
| 5 mM | 0.4342 mL | 2.1710 mL | 4.3420 mL | |
| 10 mM | 0.2171 mL | 1.0855 mL | 2.1710 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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