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

GFB-8438 

Cat. No.: HY-133012
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.

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GFB-8438 Chemical Structure

GFB-8438 Chemical Structure

CAS No. : 2304549-73-1

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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].

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].

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

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GFB-8438GFB8438GFB 8438TRP ChannelTransient receptor potential channelsmousepodocytessynaptopodinlosscytoskeletalremodelingdeoxycorticosteroneacetatesubtypeselectivekidneydiseaseInhibitorinhibitorinhibit

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