Home Cart Sign in  
HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 1336960-13-4 Chemical Structure| 1336960-13-4

Structure of GSK2193874
CAS No.: 1336960-13-4

Chemical Structure| 1336960-13-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

GSK2193874 is a selective transient receptor potential vanilloid 4 (TRPV4) blocker with IC50 value of 0.04 μM.

Synonyms: GSK2193874

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of GSK2193874

CAS No. :1336960-13-4
Formula : C37H38BrF3N4O
M.W : 691.62
SMILES Code : 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
Synonyms :
GSK2193874
MDL No. :MFCD28009510
InChI Key :UIVOZBSCHXCGPS-UHFFFAOYSA-N
Pubchem ID :53464483

Safety of GSK2193874

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301-H315-H319-H335
Precautionary Statements:P261-P301+P310-P305+P351+P338
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human lung mast cells (HLMCs) 100 nM To assess the effect of GSK1016790A on mast cells, results showed that mast cells do not express TRPV4, thus GSK1016790A had no direct effect on mast cells. PMC7330131
Human airway smooth muscle cells (HASMCs) 100 nM To assess the effect of GSK1016790A on intracellular calcium levels, results showed that GSK1016790A increased intracellular calcium but did not cause cell contraction. PMC7330131
Human alveolar epithelial cells (NCI-H441) 100 nM 3 days To test the effect of TRPV4 inhibitor GSK2193874 on IL-2 and mechanical strain-induced vascular leakage, results showed that GSK2193874 completely inhibited the increase in vascular permeability induced by IL-2 and mechanical strain. PMC8265389
Neonatal rat ventricular myocytes (NRVMs) 300 nM 48 h Pretreatment with GSK3874 reduced neurohormone-induced cardiomyocyte hypertrophy and intracellular Ca2+ concentration elevation. PMC9224988
Human vaginal epithelial cells (VK2/E6E7) 1-4μM Suppressed HSV-2 infectivity and reduced HSV-2-induced cytokine and chemokine generation PMC10042832
Rat hippocampal neurons 50-500 nM 24 h To evaluate the neuroprotective properties of GSK2193874 on NMDA-induced cytotoxicity. Results showed that GSK2193874 pretreatment significantly increased cell viability, reduced LDH release, and decreased cell death rate and intracellular calcium accumulation. PMC8275774
Atrial fibroblasts 300 nM 24 h Evaluate the effect of TRPV4 agonist on atrial fibroblast differentiation, results showed enhanced differentiation PMC7714415
Atrial myocytes 300 nM 5 min Evaluate the effect of TRPV4 agonist on action potential duration, results showed APD prolongation PMC7714415

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Guinea pigs Anesthetized guinea pigs Intraperitoneal injection 300 mg/kg Single dose, effects assessed after 1 hour To assess the inhibitory effect of GSK2193874 on bronchoconstriction induced by the TRPV4 agonist GSK1016790A, results showed that GSK2193874 significantly inhibited the bronchoconstriction caused by GSK1016790A. PMC7330131
Mice Transverse aortic constriction (TAC)-induced cardiac hypertrophy model Oral gavage 10 mg/kg Once daily for 4 weeks GSK3874 treatment significantly inhibited TAC-induced cardiac remodeling and dysfunction. PMC9224988
Rats Soman-induced status epilepticus model Intravenous injection 1 mg/kg Single dose, observed for 24 hours To evaluate the protective effects of GSK2193874 against soman-induced status epilepticus and secondary brain injury. Results showed that GSK2193874 significantly reduced seizure intensity, mortality rate, and alleviated hippocampal pathological damage. PMC8275774
Rats Sterile pericarditis model Oral gavage 30 mg/kg Once daily for 3 days Evaluate the effect of TRPV4 antagonist on atrial fibrillation susceptibility and atrial remodeling, results showed GSK2193874 significantly reduced AF vulnerability and improved atrial remodeling PMC7714415

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.45mL

0.29mL

0.14mL

7.23mL

1.45mL

0.72mL

14.46mL

2.89mL

1.45mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories