2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. GDC-0334

GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma.

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

GDC-0334 Chemical Structure

GDC-0334 Chemical Structure

CAS No. : 1984824-54-5

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Based on 1 publication(s) in Google Scholar

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Description

GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma[1][2].

IC50 & Target[2]

TRPA1

 

In Vivo

GDC-0334 (0-150 mg/kg; i.v.) decreases edema, dermal blood flow (DBF), cough, and allergic airway inflammation in rats[1].
GDC-0334 (0.5/1 mg/kg for i.v., 1/5 mg/kg mg/kg for p.o.) shows a T1/2 of 11.9 h in mice and 9.79 h in rats by i.v., and oral bioavailability (F%) of 45.0% in mice and 46.2% in rats [1].
Pharmacokinetic parameters for GDC-0334 in mouse/rat/dog/monkey [1]

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

Species IV Dose CL (ml/min/kg) VSS (liter/kg) T1/2 (h) PO Dose(mg/kg) Oral F(%)
Mouse 0.5 12.4 13.9 11.9 1 45.0
Rat 1 7.68 5.55 9.79 5 46.2
Dog 1 7.57 6.97 28.0 5 27.1
Monkey 1 14.9 5.41 7.75 5 13.4
Animal Model: Mouse, rat, dog, monkey (Pharmacokinetic assay)[2]
Dosage: 0.5,1,5 mg/kg
Administration: Intravenous injection (i.v.), oral gavage (p.o.)
Result: Showed a T1/2 of 11.9 h in mice and 9.79 h in rats by i.v., and oral bioavailability (F%) of 45.0% in mice and 46.2% in rats [1].
Animal Model: Rats/guinea pigs model of cough[2]
Dosage: 3,10,35,70,75,150 mg/kg
Administration: Intravenous injection (i.v.)
Result: Suppressed AITC-induced edema in vivo in rat.
Caused a dose-dependent reduction in AITC-induced dermal blood flow in guinea pigs.
Reduced airway airway allergic inflammation in rats and guinea pigs as well as cough in guinea pigs.
Clinical Trial
Molecular Weight

609.49

Formula

C24H19F8N5O3S
CAS No.
SMILES

O=C([C@H]1N(S(=O)(C2=CC=C(F)C=C2)=O)[C@@H](C)[C@H](F)C1)NCC3=CC(C4=CN=C(C(F)(F)F)N=C4)=NC=C3C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GDC-0334 Related Classifications

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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.

Keywords:

GDC-03341984824-54-5GDC0334GDC 0334TRP ChannelTransient receptor potential channelsRats/guinea pigs model of coughorally activeTRPA1asthmacoughallergic airway inflammationInhibitorinhibitorinhibit

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