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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.

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CAS. Nr.: 1984824-54-5
Formel: C₂₄H₁₉F₈N₅O₃S
Molecular Weight:609.49

Speicherung:

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

Data Sheet (275 KB)

GDC-0334 Chemical Structure

CAS. Nr.: 1984824-54-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

TRPA1

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

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 T_1/2 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.

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 T_1/2 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

Species	IV Dose	CL (ml/min/kg)	VSS (liter/kg)	T_1/2 (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1984824-54-5
Molecular Weight 609.49
Formel C₂₄H₁₉F₈N₅O₃S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Estrada A, et al. 1-(het)arylsulfonyl-(pyrrolidine or piperidine)-2-carboxamide derivatives and their use as trpa1 antagonists. WO2016128529 A1.

[2]. Balestrini A, et.al A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment. J Exp Med. 2021 Apr 5;218(4):e20201637. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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