GFB-8438

Cat. No.: HY-133012 Purity: 98.41%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

GFB-8438 Chemical Structure

CAS No. : 2304549-73-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 530	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TRP Channel Isoform Specific Products:

View All Isoforms

TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

hTRPC5

0.18 μM (IC₅₀)

hTRPC4

0.29 μM (IC₅₀)

rTRPC5

0.18 μM (IC₅₀)

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.

Molecular Weight

386.76

Formula

C₁₆H₁₄ClF₃N₄O₂

CAS No.

2304549-73-1

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.41%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (250 KB) LCMS (272 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

GFB-8438 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

GFB-8438

Customer Review

GFB-8438 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TRP Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

GFB-8438 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GFB-8438 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report