| Size | Price | Stock | Qty |
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| 5mg |
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| ln Vitro |
Cav3.1, Cav3.2, Cav3.3, and Cav1.2 are all blocked by apinocaltamide (Compound 66b), with IC50 values of 6.4, 18, 7.5, and 2410 nM, respectively. The recombinant channel hCav3.3 is efficiently blocked by apinocaltamide with a notable voltage dependence (Kr≈1500 nM and Ki≈20 nM). With an IC50 of 5.5 μM, apinocaltamide inhibits current flow across hKv11.1-hERG channels [1]. Moreover, apinocaltamide inhibits P450 enzymes; its IC50 values for CYP2C8, CYP2D6, CYP2C9, CYP2C19, CYP3A4, and CYP2B6 are 14, 15, 22, 25, 51, and 52 μM, respectively [1].
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| ln Vivo |
Apinocaltamide (66b, 100, and 300 mg/kg, orally administered, assessed 12 hours later) efficiently reduces the total amount of time mice experience absence-like seizures [1].
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| Animal Protocol |
Animal/Disease Models: Male juvenile DBA/2J mice (22-24 days old) [1]
Doses: 100, 300 mg/kg, 1 hour or 3 hrs (hrs (hours)) before exposure to stimulation. Route of Administration: Orally for 12 hrs (hrs (hours)) Experimental Results: Cumulative duration of absence seizures was diminished by 93% over the next 12 hrs (hrs (hours)). |
| References | |
| Additional Infomation |
Apinocaltamide is a secondary carboxamide resulting from the formal condensation of the carboxy group of {4-[1-(trifluoromethyl)cyclopropyl]phenyl}acetic acid with the amino group of 6-[(3-amino-1H-pyrazol-1-yl)methyl]pyridine-3-carbonitrile. It is a selective, orally available T-type calcium channel blocker that is being studied as a potential new treatment in epilepsy. It has a role as an anticonvulsant and a T-type calcium channel blocker. It is a member of pyrazoles, a secondary carboxamide, a member of cyclopropanes, an organofluorine compound, a nitrile, a member of pyridines and a member of benzenes.
Apinocaltamide is under investigation in clinical trial NCT03239691 (A Study to Evaluate the Effect of ACT-709478 in Photosensitive Epilepsy Patients). |
| Molecular Formula |
C22H18F3N5O
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|---|---|
| Molecular Weight |
425.40643453598
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| Exact Mass |
425.146
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| CAS # |
1838651-58-3
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| PubChem CID |
118560618
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| Appearance |
White to off-white solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
693
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LSYANGLAZUZYFX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H18F3N5O/c23-22(24,25)21(8-9-21)17-4-1-15(2-5-17)11-20(31)28-19-7-10-30(29-19)14-18-6-3-16(12-26)13-27-18/h1-7,10,13H,8-9,11,14H2,(H,28,29,31)
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| Chemical Name |
N-[1-[(5-cyanopyridin-2-yl)methyl]pyrazol-3-yl]-2-[4-[1-(trifluoromethyl)cyclopropyl]phenyl]acetamide
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| Synonyms |
ACT709478 ACT 709478ACT-709478
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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 : ≥ 125 mg/mL (~293.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 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: ≥ 2.08 mg/mL (4.89 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 20.8 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: ≥ 2.08 mg/mL (4.89 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 | 2.3507 mL | 11.7534 mL | 23.5067 mL | |
| 5 mM | 0.4701 mL | 2.3507 mL | 4.7013 mL | |
| 10 mM | 0.2351 mL | 1.1753 mL | 2.3507 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04123288 | COMPLETED | Drug: ACT-709478 Drug: ACT-709478 |
Healthy Subjects | Idorsia Pharmaceuticals Ltd. | 2019-12-16 | Phase 1 |
| NCT03165097 | COMPLETED | Drug: ACT-709478 Drug: Placebo Drug: Midazolam Drug: ACT-709478 combined with midazolam |
Healthy Subjects | Idorsia Pharmaceuticals Ltd. | 2017-07-07 | Phase 1 |
| NCT03239691 | COMPLETED | Drug: ACT-709478 for oral use Drug: Placebo |
Photosensitive Epilepsy | Idorsia Pharmaceuticals Ltd. | 2017-10-06 | Phase 2 |
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