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GSK2193874

Cat. No. M10625
GSK2193874 Structure
Synonym:

GSK-2193874; GSK2193874A

Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 147  USD147 In stock
25mg USD 287  USD287 In stock
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Quality Control
Biological Activity

GSK2193874 is a potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist with IC50 values of 2, 5, and 40 nM. It is selective for TRPV4 over ~200 other human receptors, channels, and enzymes. GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor that demonstrated ability to improve pulmonary functions in a number of heart failure models. GSK2193874 shows low clearance (7.3 mL/min/kg) and good rat oral bioavailability (31%).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 691.62
Formula C37H38BrF3N4O
CAS Number 1336960-13-4
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Mui Cheung, et al. ACS Med Chem Lett. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4

[2] Qihai David Gu, et al. Front Physiol. Activation of TRPV4 Regulates Respiration through Indirect Activation of Bronchopulmonary Sensory Neurons

[3] Kevin S Thorneloe, et al. Sci Transl Med. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure

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Keywords: GSK2193874, GSK-2193874; GSK2193874A supplier, TRP Channel, inhibitors

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