1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. GSK2193874

GSK2193874 

Cat. No.: HY-100720 Purity: 99.68%
Handling Instructions

GSK2193874 est un antagoniste oralement actif, puissant et sélectif de TRPV4 avec des IC50s de 2 nM et 40 nM pour rTRPV4 et hTRPV4.

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4.

For research use only. We do not sell to patients.

GSK2193874 Chemical Structure

GSK2193874 Chemical Structure

CAS No. : 1336960-13-4

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 128 In-stock
Estimated Time of Arrival: December 31
2 mg USD 60 In-stock
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5 mg USD 84 In-stock
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10 mg USD 144 In-stock
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25 mg USD 288 In-stock
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50 mg USD 468 In-stock
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100 mg USD 828 In-stock
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200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4[1].

IC50 & Target

IC50: 2 nM (rTRPV4), 40 nM (hTRPV4)[1]

In Vitro

GSK2193874 is profiled against TRP channels and is selective against TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8 (IC50>25 μM)[1]. GSK2193874 is a selective, orally active TRPV4 blocker that inhibits Ca2+ influx through recombinant TRPV4 channels and native endothelial TRPV4 currents. In whole-cell patch-clamp studies, GSK2193874 inhibits activation of recombinant TRPV4 currents when applied to the extracellular solution at 3 nM and above but is ineffective at up to 10 μM when applied to the inside of the cell by inclusion in the intracellular pipette solution[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

691.62

Formula

C₃₇H₃₈BrF₃N₄O

CAS No.

1336960-13-4

SMILES

O=C(C1=C(CN2CCC(N3CCCCC3)CC2)C(C4=CC=CC(C(F)(F)F)=C4)=NC5=CC(Br)=CC=C15)NC6(C7=CC=CC=C7)CC6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (144.59 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4459 mL 7.2294 mL 14.4588 mL
5 mM 0.2892 mL 1.4459 mL 2.8918 mL
10 mM 0.1446 mL 0.7229 mL 1.4459 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (3.61 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Rats[2]
Adult male Sprague-Dawley rats (n=7 to 8 per group) are treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg per day) via oral gavage for at least 4 days before osmotic challenges. Rats undergo acute and chronic hyper- and hypo-osmotic challenges. Sprague-Dawley rats are administered vehicle (0.9% NaCl, 25 mL/kg), NSC 269420 (30 mg/kg), or hydrochlorothiazide (30 mg/kg) via oral gavage. Urine is then collected over 4 hours followed by blood sampling. Rats recover for 4 days and then receive GSK2193874 (30 mg/kg per day oral gavage) for 5 days before repeating the diuretic challenge.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.68%

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Keywords:

GSK2193874GSK 2193874GSK-2193874TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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Product Name:
GSK2193874
Cat. No.:
HY-100720
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