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Apinocaltamide - 99%, high purity , Voltage-gated T-type calcium channel blocker, CAS No.1838651-58-3, Voltage-gated T-type calcium channel blocker

COA COA
In stock
Item Number
A649302
Grouped product items
SKU Size
Availability
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A649302-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$48.90
A649302-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$169.90
A649302-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$262.90
A649302-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$445.90
A649302-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$757.90
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View related series
Calcium Channel (223) Ion channel (2197) Membrane Transporter/Ion Channel (1822) Neuronal Signaling (3320)

Basic Description

Synonyms N-[1-[(5-cyanopyridin-2-yl)methyl]pyrazol-3-yl]-2-[4-[1-(trifluoromethyl)cyclopropyl]phenyl]acetamide | NBI827104 | NBI-827104 | Benzeneacetamide, N-[1-[(5-cyano-2-pyridinyl)methyl]-1H-pyrazol-3-yl]-4-[1-(trifluoromethyl)cyclopropyl]-
Specifications & Purity Moligand™, ≥99%
Biochemical and Physiological Mechanisms 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.
Storage Temp Store at -20°C,Argon charged
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type BLOCKER
Mechanism of action Voltage-gated T-type calcium channel blocker
Product Description

Apinocaltamide (ACT-709478) is a potent, selective brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Phenylacetamides
Intermediate Tree Nodes Not available
Direct Parent Phenylacetamides
Alternative Parents N-arylamides  3-pyridinecarbonitriles  Imidolactams  Pyrazoles  Heteroaromatic compounds  Secondary carboxylic acid amides  Nitriles  Azacyclic compounds  Organopnictogen compounds  Organofluorides  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  Alkyl fluorides  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Phenylacetamide - 3-pyridinecarbonitrile - N-arylamide - Imidolactam - Pyridine - Heteroaromatic compound - Pyrazole - Azole - Secondary carboxylic acid amide - Carboxamide group - Azacycle - Organoheterocyclic compound - Nitrile - Carbonitrile - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Carbonyl group - Alkyl halide - Alkyl fluoride - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as phenylacetamides. These are amide derivatives of phenylacetic acids.
External Descriptors Not available

Product Properties

ALogP 3.3

Associated Targets(Human)

CACNA1H Tclin Voltage-dependent T-type calcium channel subunit alpha-1H (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CACNA1G Tclin Voltage-dependent T-type calcium channel subunit alpha-1G (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CACNA1I Tclin Voltage-dependent T-type calcium channel subunit alpha-1I (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CACNA1C Tclin Voltage-dependent L-type calcium channel subunit alpha-1C (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CACNA1H Tclin Voltage-gated T-type calcium channel alpha-1H subunit (1913 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SCN1A Tclin Sodium channel protein type I alpha subunit (483 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CASR Tclin Calcium sensing receptor (766 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TACR2 Tchem Neurokinin 2 receptor (3341 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNA5 Tclin Voltage-gated potassium channel subunit Kv1.5 (1353 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
UTS2R Tchem Urotensin II receptor (1388 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SCN5A Tclin Sodium channel protein type V alpha subunit (3462 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CACNA1A Tchem Voltage-gated P/Q-type calcium channel alpha-1A subunit (4 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LPAR3 Tchem Lysophosphatidic acid receptor Edg-7 (471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2A6 Tchem Cytochrome P450 2A6 (2861 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NMUR1 Tchem Neuromedin-U receptor 1 (374 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HCN4 Tclin Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (92 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNQ1 Tclin Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) (185 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNQ2 Tclin Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3) (372 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNJ3 Tchem Kir3.1/Kir3.4 (583 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCND3 Tclin Kv channel-interacting protein 2/Potassium voltage-gated channel subfamily D member 3 (9 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Sigmar1 Sigma opioid receptor (160 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cacna1d Voltage-gated L-type calcium channel alpha-1D subunit (336 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Scn2a Sodium channel protein type II alpha subunit (191 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Scn8a Sodium channel protein type VIII alpha subunit (53 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cacna1g Voltage-gated T-type calcium channel alpha-1G subunit (1 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cacna1i Voltage-gated T-type calcium channel alpha-1I subunit (2 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Salmonella typhimurium (15756 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cavia porcellus (23802 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cynomolgus monkey (4946 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Kcnj2 Inward rectifier potassium channel 2 (11 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cacna1h Voltage-dependent T-type calcium channel subunit alpha-1H (2 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name N-[1-[(5-cyanopyridin-2-yl)methyl]pyrazol-3-yl]-2-[4-[1-(trifluoromethyl)cyclopropyl]phenyl]acetamide
INCHI 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)
InChIKey LSYANGLAZUZYFX-UHFFFAOYSA-N
Smiles C1CC1(C2=CC=C(C=C2)CC(=O)NC3=NN(C=C3)CC4=NC=C(C=C4)C#N)C(F)(F)F
Isomeric SMILES C1CC1(C2=CC=C(C=C2)CC(=O)NC3=NN(C=C3)CC4=NC=C(C=C4)C#N)C(F)(F)F
Alternate CAS 1838651-58-3
PubChem CID 118560618
MeSH Entry Terms ACT-709478;N-(1-((5-cyanopyridin-2-yl)methyl)pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide
Molecular Weight 425.41

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : ≥ 125 mg/mL (293.83 mM)
Molecular Weight 425.400 g/mol
XLogP3 3.300
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 6
Exact Mass 425.146 Da
Monoisotopic Mass 425.146 Da
Topological Polar Surface Area 83.600 Ų
Heavy Atom Count 31
Formal Charge 0
Complexity 693.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Alternative Products

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    Apinocaltamide, Voltage-gated T-type calcium channel blocker
    • 10mM in DMSO

    Starting at $576.90

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