1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. GFB-8438

GFB-8438 

Cat. No.: HY-133012 Purity: 98.07%
Handling Instructions

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

GFB-8438 Chemical Structure

CAS No. : 2304549-73-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 308 In-stock
Estimated Time of Arrival: December 31
5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

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[1].

IC50 & Target[1]

hTRPC5

0.18 μM (IC50)

hTRPC4

0.29 μM (IC50)

rTRPC5

0.18 μM (IC50)

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].

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 Cl, VSS, and  t1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hours, respectively[1].

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 Cl, Vss,  and t1/2 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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (215.46 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

GFB-8438GFB8438GFB 8438TRP ChannelTransient receptor potential channelsmousepodocytessynaptopodinlosscytoskeletalremodelingdeoxycorticosteroneacetatesubtypeselectivekidneydiseaseInhibitorinhibitorinhibit

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GFB-8438
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