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GSK2193874

Cat. No. M10625
GSK2193874 Structure
Synonym:

GSK-2193874; GSK2193874A

Size Price Availability Quantity
5mg USD 72  USD72 In stock
10mg USD 128  USD128 In stock
25mg USD 238  USD238 In stock
50mg USD 445  USD445 In stock
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Quality Control & Documentation
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%).

Chemical Information
Molecular Weight 691.62
Formula C37H38BrF3N4O
CAS Number 1336960-13-4
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] 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, activators


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