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GSK205

Cat. No. M14279
GSK205 Structure
Size Price Availability Quantity
10mg USD 330  USD330 In stock
25mg USD 700  USD700 In stock
50mg USD 1180  USD1180 In stock
100mg USD 1950  USD1950 In stock
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Quality Control & Documentation
Biological Activity

GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca2+ influx.

Chemical Information
Molecular Weight 481.45
CAS Number 1263068-83-2
Solubility (25°C) DMSO 150 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] S Fu, et al. Activation of TRPV4 by mechanical, osmotic or pharmaceutical stimulation is anti-inflammatory blocking IL-1β mediated articular cartilage matrix destruction

[2] Yun Shen, et al. The roles of mechanosensitive ion channels and associated downstream MAPK signaling pathways in PDLC mechanotransduction

[3] Patrick Kanju, et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain

[4] Lauren Hurd, et al. A mutation in TRPV4 results in altered chondrocyte calcium signaling in severe metatropic dysplasia

[5] Mimi N Phan, et al. Functional characterization of TRPV4 as an osmotically sensitive ion channel in porcine articular chondrocytes

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  Catalog
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Keywords: GSK205 supplier, TRP Channel, inhibitors, activators

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