1. Membrane Transporter/Ion Channel
  2. TRP Channel

Pico145 (Synonyms: HC-608)

Cat. No.: HY-101507 Purity: 99.42%
Handling Instructions

Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

For research use only. We do not sell to patients.

Pico145 Chemical Structure

Pico145 Chemical Structure

CAS No. : 1628287-16-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 404 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.

IC50 & Target

IC50: 0.349 nM (TRPC4, cell assay), 1.3 nM (TRPC5, cell assay), 0.03 nM (TRPC4-TRPC1, cell assay), 0.2 nM (TRPC5-TRPC1, cell assay)[1]

In Vitro

Pico145 (Compound 31, C31) is a remarkable small-molecule inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells; Pico145 shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. 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). The potency of Pico145 can be reduced by increased (−)-englerin A concentration. Furthermore, Pico145 potently inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P), and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels with an IC50 of 0.011 nM. 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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (238.15 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9052 mL 9.5260 mL 19.0520 mL
5 mM 0.3810 mL 1.9052 mL 3.8104 mL
10 mM 0.1905 mL 0.9526 mL 1.9052 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Cells are seeded at 90% confluence into 96-well clear-bottomed poly-d-lysine-coated black plates for HEK 293 cells and clear-bottomed Nunc plates for A498 cells, Hs578T cells, and HUVECs 24 h before experimentation. Fura-2 Ca2+ indicator dye is used to monitor changes in intracellular ionized Ca2+ concentration. To perform the experiment, the cells are incubated for 1 h with fura-2-AM (2 μM) in standard bath solution (SBS) at 37°C in the presence of 0.01% pluronic acid. SBS contains 135 mM NaCl, 5 mM KCl, 1.2 mM MgCl2, 1.5 mM CaCl2, 8 mM glucose, and 10 mM Hepes (pH titrated to 7.4 using NaOH). Subsequently, the cells are washed twice with SBS before adding Pico145 or ML204 for 30 min before making Ca2+ measurements. The fura-2 fluorescence is recorded using a 96-well fluorescence plate reader and the excitation wavelengths of 340 and 380 nm. For TRPV4 recordings, fluo-4/AM is used in place of fura-2/AM, and 2.5 mM probenecid is included to inhibit leak of fluo-4. Fluo-4 is excited at 485 nm, and emitted light is collected at 525 nm. Ca2+ is indicated by the ratio of the fluorescence (F) emission intensities for the two excitation wavelengths. Measurements are made at room temperature (21 ± 3°C)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

524.88

Formula

C₂₃H₂₀ClF₃N₄O₅

CAS No.

1628287-16-0

SMILES

O=C1C2=C(N=C(OC3=CC=CC(OC(F)(F)F)=C3)N2CC4=CC=C(Cl)C=C4)N(C)C(N1CCCO)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Pico145
Cat. No.:
HY-101507
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Pico145

Cat. No.: HY-101507