ACT 709478
- Product Name
- ACT 709478
- CAS No.
- 1838651-58-3
- Chemical Name
- ACT 709478
- Synonyms
- ACT 709478;apinocaltamide;ACT-709478 1838651-58-3;ACT 709478 (ACT709478);N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide;Benzeneacetamide, N-[1-[(5-cyano-2-pyridinyl)methyl]-1H-pyrazol-3-yl]-4-[1-(trifluoromethyl)cyclopropyl]-
- CBNumber
- CB34667491
- Molecular Formula
- C22H18F3N5O
- Formula Weight
- 425.41
- MOL File
- 1838651-58-3.mol
ACT 709478 Property
- Boiling point:
- 646.4±55.0 °C(Predicted)
- Density
- 1.36±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:125.0(Max Conc. mg/mL);293.83(Max Conc. mM)
- form
- A solid
- pka
- 13.52±0.70(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- API0045909
- Product name
- ACT-709478
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $459.16
- Updated
- 2021/12/16
- Product number
- CS-0062884
- Product name
- ACT-709478
- Purity
- 99.68%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0062884
- Product name
- ACT-709478
- Purity
- 99.68%
- Packaging
- 10mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- CS-0062884
- Product name
- ACT-709478
- Purity
- 99.68%
- Packaging
- 50mg
- Price
- $2750
- Updated
- 2021/12/16
- Product number
- CS-0062884
- Product name
- ACT-709478
- Purity
- 99.68%
- Packaging
- 100mg
- Price
- $3950
- Updated
- 2021/12/16
ACT 709478 Chemical Properties,Usage,Production
Uses
Apinocaltamide (ACT-709478) is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies[1].
Definition
ChEBI: 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.
in vivo
Apinocaltamide (Compound 66b, 100, 300 mg/kg, p.o., measured 12 hours later) potently decreases the cumulative duration of absence-like seizures in mice[1].
| Animal Model: | Male juvenile DBA/2J mice (22-24 days old)[1] |
| Dosage: | 100, 300 mg/kg, 1 hour or 3 hours before exposure to the stimulus. |
| Administration: | P.O., for 12 hours |
| Result: | Decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%. |
IC 50
Cav1.2: 2410 nM (IC50); CaV3.1: 6.4 nM (IC50); Cav3.2: 18 nM (IC50); CaV3.3: 7.5 nM (IC50)
References
[1] Bezen?on O, et al. Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. J Med Chem. 2017 Dec 14;60(23):9769-9789. DOI:10.1021/acs.jmedchem.7b01236
ACT 709478 Preparation Products And Raw materials
Raw materials
Preparation Products
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