Art. -Nr.: HY-101507

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(Synonyms: Pico145; HC-608)

13 Cited Publications

Kundenbewertung

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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Reinheit: 99.47%
CAS. Nr.: 1628287-16-0
Formel: C₂₃H₂₀ClF₃N₄O₅
Molecular Weight:524.88

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Zerencotrep Chemical Structure

CAS. Nr.: 1628287-16-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.012 nM Compound: 12; HC-608, Pico-145	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	[PMID: 30943030]
HEK293	IC₅₀	0.03 nM Compound: 12; HC-608, Pico-145	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	[PMID: 30943030]
HEK293	IC₅₀	0.033 nM Compound: 12; HC-608, Pico-145	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	[PMID: 30943030]
HEK293	IC₅₀	0.19 nM Compound: 12; HC-608, Pico-145	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	[PMID: 30943030]
HEK293	IC₅₀	0.34 nM Compound: 12; HC-608, Pico-145	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	[PMID: 30943030]
HEK293	IC₅₀	1.3 nM Compound: 12; HC-608, Pico-145	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	[PMID: 30943030]

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].

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

Chemical Information

CAS. Nr. 1628287-16-0
Appearance Solid
Molecular Weight 524.88
Formel C₂₃H₂₀ClF₃N₄O₅
Color White to off-white
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
Synonyms

Pico145; HC-608
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Nat Commun

Ultrasound-mediated spatial and temporal control of engineered cells in vivo. [Abstract]

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

Reduction of TRPC1/TRPC3 mediated Ca2+-signaling protects oxidative stress-induced COPD. [Abstract]

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
The Medical College of Wisconsin

2025.
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
bioRxiv

2023 Jul 2.

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Rubaiy HN, et al. Picomolar, selective, and subtype-specific small-molecule inhibition of TRPC1/4/5 channels. J Biol Chem. 2017 May 19;292(20):8158-8173. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Zerencotrep

13 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Zerencotrep

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zerencotrep

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Zerencotrep

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zerencotrep Related Classifications

HY-101507 Related Classifications