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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- No. CAS: 1984824-54-5
- Fòrmula: C24H19F8N5O3S
- Peso molecular:609.49
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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TRPA1 |
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]
| 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 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1984824-54-5
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Peso molecular 609.49
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Fòrmula C24H19F8N5O3S
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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