Art. -Nr.: HY-133012

GFB-8438

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GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.

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Reinheit: 99.74%
CAS. Nr.: 2304549-73-1
Formel: C₁₆H₁₄ClF₃N₄O₂
Molecular Weight:386.76

Speicherung:

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

GFB-8438 Chemical Structure

CAS. Nr.: 2304549-73-1

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

hTRPC5

0.18 μM (IC₅₀)

hTRPC4

0.29 μM (IC₅₀)

rTRPC5

0.18 μM (IC₅₀)

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>30 μM Compound: GFB-8438	Inhibition of human Nav1.5 stably expressed in CHO cells measured at holding potential of -80 mV by manual patch clamp assay Inhibition of human Nav1.5 stably expressed in CHO cells measured at holding potential of -80 mV by manual patch clamp assay	[PMID: 31749913]
HEK293	IC₅₀	>30 μM Compound: GFB-8438	Inhibition of OAG-activated human TRPC6 channel expressed in HEK293 cells by Q-patch clamp assay Inhibition of OAG-activated human TRPC6 channel expressed in HEK293 cells by Q-patch clamp assay	[PMID: 31749913]
HEK293	IC₅₀	0.18 μM Compound: GFB-8438	Inhibition of rosiglitazone-activated human TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay Inhibition of rosiglitazone-activated human TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay	[PMID: 31749913]
HEK293	IC₅₀	0.18 μM Compound: GFB-8438	Inhibition of rosiglitazone-activated rat TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay Inhibition of rosiglitazone-activated rat TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay	[PMID: 31749913]
HEK293	IC₅₀	0.28 μM Compound: GFB-8438	Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as decrease in current amplitude treated for 3 mins measured between +80 mV and -80 mV by manual patch clamp assay Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as decrease in current amplitude treated for 3 mins measured between +80 mV and -80 mV by manual patch clamp assay	[PMID: 31749913]
HEK293	IC₅₀	0.29 μM Compound: GFB-8438	Inhibition of Englerin-activated human TRPC4 channel expressed in HEK293 cells by Q-patch clamp assay Inhibition of Englerin-activated human TRPC4 channel expressed in HEK293 cells by Q-patch clamp assay	[PMID: 31749913]
HEK293	IC₅₀	8.7 μM Compound: GFB-8438	Inhibition of human ERG stably expressed in HEK293 cells measured at holding potential of -90 mV by manual patch clamp assay Inhibition of human ERG stably expressed in HEK293 cells measured at holding potential of -90 mV by manual patch clamp assay	[PMID: 31749913]

In Vitro

Pretreatment of mouse podocyte with GFB-8438 (1 μM for 30 min), followed by incubation with protamine sulfate, effectively blocked synaptopodin loss and cytoskeletal remodeling^[1].

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

In Vivo

GFB-8438 (30 mg/kg; s.c.; daily for 3 weeks) is efficacious in a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of focal segmental glomerulosclerosis (FSGS), significantly reducing both total protein and albumin concentrations in urine^[1].
GFB-8438 (1 mg/kg; i.v.) treatment shows the?C_l,?V_SS,?and ?t_1/2?were?31?mL/min/kg,?1.17?L/kg,?and?0.5 hours, respectively^[1].

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

Animal Model:

Sprague Dawley rats (DOCA-salt rat model of FSGS)^[1]
Dosage:

30 mg/kg
Administration:

s.c.; daily for 3 weeks
Result:

Significant reduction in urine protein concentrations.

Animal Model:

6-8 weeks old male SD rats^[1]
Dosage:

1 mg/kg
Administration:

i.v. (Pharmacokinetic Analysis)
Result:

The C_l, V_ss, and t_1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hours, respectively.

Chemical Information

CAS. Nr. 2304549-73-1
Appearance Solid
Molecular Weight 386.76
Formel C₁₆H₁₄ClF₃N₄O₂
Color Off-white to light yellow
SMILES

O=C1CN(C2=C(Cl)C(NN=C2)=O)CCN1CC3=CC=CC=C3C(F)(F)F
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 83.33 mg/mL (215.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.5856 mL

12.9279 mL

25.8558 mL

5 mM

0.5171 mL

2.5856 mL

5.1712 mL

10 mM

0.2586 mL

1.2928 mL

2.5856 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: ≥ 2.08 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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]. Yu M, et al.Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.ACS Med Chem Lett. 2019 Oct 22;10(11):1579-1585. [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	2.5856 mL	12.9279 mL	25.8558 mL	64.6396 mL
	5 mM	0.5171 mL	2.5856 mL	5.1712 mL	12.9279 mL
	10 mM	0.2586 mL	1.2928 mL	2.5856 mL	6.4640 mL
	15 mM	0.1724 mL	0.8619 mL	1.7237 mL	4.3093 mL
	20 mM	0.1293 mL	0.6464 mL	1.2928 mL	3.2320 mL
	25 mM	0.1034 mL	0.5171 mL	1.0342 mL	2.5856 mL
	30 mM	0.0862 mL	0.4309 mL	0.8619 mL	2.1547 mL
	40 mM	0.0646 mL	0.3232 mL	0.6464 mL	1.6160 mL
	50 mM	0.0517 mL	0.2586 mL	0.5171 mL	1.2928 mL
	60 mM	0.0431 mL	0.2155 mL	0.4309 mL	1.0773 mL
	80 mM	0.0323 mL	0.1616 mL	0.3232 mL	0.8080 mL
	100 mM	0.0259 mL	0.1293 mL	0.2586 mL	0.6464 mL

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GFB-8438

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GFB-8438

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GFB-8438 Related Classifications

HY-133012 Related Classifications