| Identification | Back Directory | [Name]
3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide | [CAS]
1336960-13-4 | [Synonyms]
GSK2193874
GSK 2193874; GSK2193874
GSK2193874 >=98% (HPLC)
TRPV4 antagonist GS2193874
3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
4-Quinolinecarboxamide, 3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]- | [Molecular Formula]
C37H38BrF3N4O | [MDL Number]
MFCD28009510 | [MOL File]
1336960-13-4.mol | [Molecular Weight]
691.62 |
| Chemical Properties | Back Directory | [Boiling point ]
737.8±60.0 °C(Predicted) | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
12.82±0.20(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
GSK 2193874 is an orally active, potent and selective TRPV4 antagonist. | [Uses]
GSK2193874 has been used as a transient receptor potential vanilloid 4 (TRPV4) antagonist:
- to study its effects on GSK101-induced colon contractions in mice
- to study its effects on murine compact bone-derived osteoblasts(CB-OB)
- to study its effects on lung injury post-lipopolysaccharide (LPS) in mice
| [Biochem/physiol Actions]
GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC50 = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model. | [in vivo]
The pharmacokinetic (PK) properties for GSK2193874 are evaluated in both rat and dog and found to have half-lives and oral exposure suitable for oral dosing in chronic animal models (Rat PK: iv CL=7.3 mL/min/kg, po t1/2=10 h, %F=31. Dog PK: iv CL=6.9 mL/min/kg, po t1/2=31 h, %F=53). In addition, GSK2193874 shows no blood pressure or heart rate effect in rats when dose up to 30 mg/kg. GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor that demonstrated ability to improve pulmonary functions in a number of heart failure models[1]. GSK2193874 shows low clearance (7.3 mL/min/kg) and good rat oral bioavailability (31%)[2]. | [storage]
Store at +4°C |
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| Company Name: |
Sigma-Aldrich
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021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
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