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Pico145

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Catalog No. T16532Cas No. 1628287-16-0
Alias HC-608

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

Pico145

Pico145

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Purity: 99.06%
Catalog No. T16532Alias HC-608Cas No. 1628287-16-0
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$67In StockIn Stock
5 mg$162In StockIn Stock
10 mg$238In StockIn Stock
25 mg$397In StockIn Stock
50 mg$575In StockIn Stock
100 mg$786In StockIn Stock
200 mg$1,120-In Stock
1 mL x 10 mM (in DMSO)$186In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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.
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Purity:99.06%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.
Targets&IC50
TRPC4-TRPC1:0.03 nM (cell assay), TRPC5-TRPC1:0.2 nM (cell assay), TRPC4:0.349 nM (cell assay), TRPC5:1.3 nM (cell assay)
In vitro
Pico145 is a remarkable small-molecule inhibitor of TRPC1/4/5 channels. Pico145 displays no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells). Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers expressed in HEK 293 Tet+ cells (IC50, 0.03 nM, and 0.2 nM, respectively). Pico145 effectively inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P) and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels (IC50: 0.011 nM). The potency of Pico145 can be reduced by increased (?)-englerin A concentration. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC50, 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca2+ entry and histamine-evoked Ca2+ entry into endothelial cells[1].
SynonymsHC-608
Chemical Properties
Molecular Weight524.88
FormulaC23H20ClF3N4O5
Cas No.1628287-16-0
SmilesCn1c2nc(Oc3cccc(OC(F)(F)F)c3)n(Cc3ccc(Cl)cc3)c2c(=O)n(CCCO)c1=O
Relative Density.1.48 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 71.43 mg/mL (136.09 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.29 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9052 mL9.5260 mL19.0520 mL95.2599 mL
5 mM0.3810 mL1.9052 mL3.8104 mL19.0520 mL
10 mM0.1905 mL0.9526 mL1.9052 mL9.5260 mL
20 mM0.0953 mL0.4763 mL0.9526 mL4.7630 mL
50 mM0.0381 mL0.1905 mL0.3810 mL1.9052 mL
100 mM0.0191 mL0.0953 mL0.1905 mL0.9526 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

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