Shopping Cart
  • Remove All
  • TargetMol
    Your shopping cart is currently empty

Apinocaltamide

🥰Excellent
Catalog No. T14120Cas No. 1838651-58-3
Alias NBI827104, NBI 827104, ACT-709478, ACT709478

Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.

Apinocaltamide

Apinocaltamide

🥰Excellent
Purity: 99.80%
Catalog No. T14120Alias NBI827104, NBI 827104, ACT-709478, ACT709478Cas No. 1838651-58-3
Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.
Pack SizePriceAvailabilityQuantity
2 mg$89In Stock
5 mg$178In Stock
Add to Cart
Add to Quotation
Bulk & Custom
Questions
View More
Select Batch
Purity:99.80%
Contact us for more batch information
Resource Download
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Product Introduction

Bioactivity
Description
Apinocaltamide (ACT-709478) is an orally available and selective T-type calcium channel blocker that penetrates the blood-brain barrier (BBB) with IC50=6.4-18nM for Cav3.1, Cav3.2, and Cav3.3, and is commonly used in epilepsy research.
Targets&IC50
CYP2C8:14 μM, CYP2C9:22 μM, CYP3A4:51 μM, Cav 3.1:6.4 nM, hKv11.1-hERG:5.5 μM, Cav 3.2:18 nM, CYP2C19:25 μM, Cav 1.2:2410 nM, CYP2B6:52 μM, CYP2D6:15 μM, Cav 3.3:7.5 nM
In vitro
Apinocaltamide (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. Apinocaltamide also inhibits P450 enzymes with IC50s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively[1]. Apinocaltamide blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM[1]. Apinocaltamide blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM)[1].
In vivo
In male juvenile DBA/2J mice (22–24 days old), oral administration of Apinocaltamide (100 or 300 mg/kg, given 1 or 3 hours prior to stimulation) significantly reduced the cumulative duration of absence-like seizures over the following 12 hours by 93%, indicating strong anti-absence seizure efficacy[1].
AliasNBI827104, NBI 827104, ACT-709478, ACT709478
Chemical Properties
Molecular Weight425.41
FormulaC22H18F3N5O
Cas No.1838651-58-3
SmilesN#CC1=CN=C(C=C1)CN2N=C(C=C2)NC(=O)CC3=CC=C(C=C3)C4(CC4)C(F)(F)F
Relative Density.1.36 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 120 mg/mL (282.08 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3507 mL11.7534 mL23.5067 mL117.5337 mL
5 mM0.4701 mL2.3507 mL4.7013 mL23.5067 mL
10 mM0.2351 mL1.1753 mL2.3507 mL11.7534 mL
20 mM0.1175 mL0.5877 mL1.1753 mL5.8767 mL
50 mM0.0470 mL0.2351 mL0.4701 mL2.3507 mL
100 mM0.0235 mL0.1175 mL0.2351 mL1.1753 mL

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Sci Citations

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

Related Tags: buy Apinocaltamide | purchase Apinocaltamide | Apinocaltamide cost | order Apinocaltamide | Apinocaltamide chemical structure | Apinocaltamide in vivo | Apinocaltamide in vitro | Apinocaltamide formula | Apinocaltamide molecular weight