A TRPC5 inhibitor
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GFB-8438

Item No. 43035

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-chloro-5-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]-1-piperazinyl]-3(2H)-pyridazinone
CAS Number
2304549-73-1
Molecular Formula
C16H14ClF3N4O2
Formula Weight
386.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
FC(F)(C1=C(CN2CCN(C(C=NNC3=O)=C3Cl)CC2=O)C=CC=C1)F
InChi Code
InChI=1S/C16H14ClF3N4O2/c17-14-12(7-21-22-15(14)26)23-5-6-24(13(25)9-23)8-10-3-1-2-4-11(10)16(18,19)20/h1-4,7H,5-6,8-9H2,(H,22,26)
InChi Key
MITRKIWBJVJRAM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $91

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    10 mg

    $168

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    50 mg

    $396

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    100 mg

    $616

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    Product Description

    GFB-8438 is an inhibitor of transient receptor potential canonical 5 (TRPC5; IC50 = 0.18 µM).1 It is selective for TRPC5 over TRPC6 and voltage-gated sodium channel 1.5 (Nav1.5; IC50s = >30 µM for both) and a panel of 100 receptors and kinases at 10 µM but does inhibit TRPC4 (IC50 = 0.29 µM). GFB-8438 (30 mg/kg per day) decreases urinary excretion of total protein and albumin in a rat model of high salt- and unilateral nephrectomy-induced renal hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yu, M., Ledeboer, M.W., Daniels, M., et al. Discovery of a potent and selective TRPC5 inhibitor, efficacious in a focal segmental glomerulosclerosis model. ACS Med. Chem. Lett. 10(11), 1579-1585 (2019).