GSK2193874
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
500mg | $1420 | Check With Us |
1g | $2100 | Check With Us |
5g | $5670 | Check With Us |
Cat #: V3556 CAS #: 1336960-13-4 Purity ≥ 98%
Description: GSK2193874 (GSK-2193874) is a novel, potent, orally bioactive, and selective TRPV4 (Transient Receptor Potential Vanilloid 4) antagonist with the potential to be used for congestive heart failure.
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Molecular Weight (MW) | 691.62 |
---|---|
Molecular Formula | C37H38BrF3N4O |
CAS No. | 1336960-13-4 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent |
Protocol | In Vitro | GSK2193874 is profiled against TRP channels and is selective against TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8 (IC50>25 μM) |
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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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.4459 mL | 7.2294 mL | 14.4588 mL | 28.9176 mL |
5mM | 0.2892 mL | 1.4459 mL | 2.8918 mL | 5.7835 mL |
10mM | 0.1446 mL | 0.7229 mL | 1.4459 mL | 2.8918 mL |
20mM | 0.0723 mL | 0.3615 mL | 0.7229 mL | 1.4459 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.