Zerencotrep
Based on 13 publication(s) in Google Scholar
Pico145 (HC-608) 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.
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- Pureté: 99.47%
- CAS No.: 1628287-16-0
- Formule: C23H20ClF3N4O5
- Masse moléculaire:524.88
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
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Publications Citing Use of MedChemExpress (MCE) Zerencotrep
More- Nat Commun. 2024 Aug 27;15(1):7369. [Abstract]
- Cell Rep. 2025 Sep 22;44(10):116308. [Abstract]
- Mol Metab. 2022 Dec:66:101645. [Abstract]
- Cell Mol Life Sci. 2024 Aug 29;81(1):374. [Abstract]
- Cell Signal. 2023 Jul:107:110681. [Abstract]
- Food Chem Toxicol. 2019 Jul:129:281-290. [Abstract]
- Oral Dis. 2025 Mar;31(3):918-927. [Abstract]
- PLoS One. 2021 Apr 23;16(4):e0250095. [Abstract]
- Behav Brain Res. 2022 Apr 9:423:113765. [Abstract]
- Biochem Biophys Res Commun. 2025 Nov 1:787:152776. [Abstract]
- The Medical College of Wisconsin. 2025.
- bioRxiv. 2024 Dec 23:2024.12.23.629519. [Abstract]
- bioRxiv. 2023 Jul 2.
Activité biologique
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]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.012 nM
Compound: 12; HC-608, Pico-145
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Inhibition of human TRPC4 expressed in HEK293 cells assessed as reduction in sphingosine-1-phosphate-induced current at -100 mV by patch clamp assay
Inhibition of human TRPC4 expressed in HEK293 cells assessed as reduction in sphingosine-1-phosphate-induced current at -100 mV by patch clamp assay
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[PMID: 30943030] |
| HEK293 | IC50 |
0.03 nM
Compound: 12; HC-608, Pico-145
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Inhibition of human TRPC4 expressed in HEK293 cells assessed as reduction in sphingosine-1-phosphate-induced current at +100 mV by patch clamp assay
Inhibition of human TRPC4 expressed in HEK293 cells assessed as reduction in sphingosine-1-phosphate-induced current at +100 mV by patch clamp assay
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[PMID: 30943030] |
| HEK293 | IC50 |
0.033 nM
Compound: 12; HC-608, Pico-145
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Inhibition of human TRPC4/human TRPC1 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
Inhibition of human TRPC4/human TRPC1 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
0.19 nM
Compound: 12; HC-608, Pico-145
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Inhibition of human TRPC5/human TRPC1 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
Inhibition of human TRPC5/human TRPC1 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
0.34 nM
Compound: 12; HC-608, Pico-145
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Inhibition of human TRPC4 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
Inhibition of human TRPC4 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 30943030] |
| HEK293 | IC50 |
1.3 nM
Compound: 12; HC-608, Pico-145
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Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in englerin A-induced calcium entry incubated for 30 mins by Fluo-4AM dye based fluorescence assay
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[PMID: 30943030] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1628287-16-0
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Appearance Solid
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Masse moléculaire 524.88
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Formule C23H20ClF3N4O5
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Color White to off-white
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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
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Synonyms
Pico145; HC-608
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
2024 Aug 27;15(1):7369. PMID: 39191796 -
Cell Rep
Mechanosensitive calcium channels and integrins coordinate the reprogramming of colorectal cancer cells into a fetal-like state. [Abstract]2025 Sep 22;44(10):116308. PMID: 40986425 -
Mol Metab
CRISPR/SaCas9 mutagenesis of stromal interaction molecule 1 in proopiomelanocortin neurons increases glutamatergic excitability and protects against diet-induced obesity. [Abstract]2022 Dec:66:101645. PMID: 36442744 -
Cell Mol Life Sci
Functional determinants of lysophospholipid- and voltage-dependent regulation of TRPC5 channel. [Abstract]2024 Aug 29;81(1):374. PMID: 39210039 -
Cell Signal
2023 Jul:107:110681. PMID: 37062436 -
Food Chem Toxicol
Activation of TRPC6 channels contributes to (+)-conocarpan-induced apoptotic cell death in HK-2 cells. [Abstract]2019 Jul:129:281-290. PMID: 31054997 -
Oral Dis
Stretched Vascular Endothelial Cells Polarized Neutrophils to N2 Type via TRPC1-IL13-STAT3 Axis. [Abstract]2025 Mar;31(3):918-927. PMID: 39462789 -
PLoS One
Impact of Na+ permeation on collective migration of pulmonary arterial endothelial cells. [Abstract]2021 Apr 23;16(4):e0250095. PMID: 33891591 -
Behav Brain Res
Inhibition of TRPC1, TRPM4 and CHRNA6 ion channels ameliorates depression-like behavior in rats. [Abstract]2022 Apr 9:423:113765. PMID: 35063497 -
Biochem Biophys Res Commun
Non-Ser36 phosphorylated p66Shc inhibits TRPC-dependent and TRPC-independent calcium influx in vascular smooth muscle cells. [Abstract]2025 Nov 1:787:152776. PMID: 41086682 -
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bioRxiv
Angiotensin II elicits robust calcium oscillations coordinated within juxtaglomerular cell clusters to suppress renin secretion. [Abstract]2024 Dec 23:2024.12.23.629519. PMID: 39763801 -
Solvant et solubilité
DMSO : ≥ 100 mg/mL (190.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9052 mL | 9.5260 mL | 19.0520 mL | 47.6299 mL |
| 5 mM | 0.3810 mL | 1.9052 mL | 3.8104 mL | 9.5260 mL | |
| 10 mM | 0.1905 mL | 0.9526 mL | 1.9052 mL | 4.7630 mL | |
| 15 mM | 0.1270 mL | 0.6351 mL | 1.2701 mL | 3.1753 mL | |
| 20 mM | 0.0953 mL | 0.4763 mL | 0.9526 mL | 2.3815 mL | |
| 25 mM | 0.0762 mL | 0.3810 mL | 0.7621 mL | 1.9052 mL | |
| 30 mM | 0.0635 mL | 0.3175 mL | 0.6351 mL | 1.5877 mL | |
| 40 mM | 0.0476 mL | 0.2381 mL | 0.4763 mL | 1.1907 mL | |
| 50 mM | 0.0381 mL | 0.1905 mL | 0.3810 mL | 0.9526 mL | |
| 60 mM | 0.0318 mL | 0.1588 mL | 0.3175 mL | 0.7938 mL | |
| 80 mM | 0.0238 mL | 0.1191 mL | 0.2381 mL | 0.5954 mL | |
| 100 mM | 0.0191 mL | 0.0953 mL | 0.1905 mL | 0.4763 mL |
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