1. Membrane Transporter/Ion Channel
  2. Calcium Channel

GSK-7975A 

Cat. No.: HY-12507 Purity: 99.56%
Handling Instructions

GSK-7975A is a potent and orally available CRAC channel inhibitor.

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

GSK-7975A Chemical Structure

GSK-7975A Chemical Structure

CAS No. : 1253186-56-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
25 mg USD 410 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK-7975A is a potent and orally available CRAC channel inhibitor.

In Vitro

GSK-7975A reduces FcεRI-dependent Ca2+ influx and 3 μM GSK-7975A reduces the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50%[1]. GSK-7975A inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety species. GSK-7975A completely inhibits calcium influx through CRAC channels. This leads to inhibition of the release of mast cell mediators and T-cell cytokines from multiple human and rat preparations. Mast cells from guinea-pig and mouse preparations are not inhibited by GSK-7975A; however cytokine release is fully blocked from T-cells in a mouse preparation[2]. GSK-7975A inhibits toxin-induced activation of ORAI1 and/or activation of Ca2+ currents after Ca2+ release, in a concentration-dependent manner, in mouse and human pancreatic acinar cells (inhibition >90% of the levels observed in control cells). GSK-7975A also prevents activation of the necrotic cell death pathway in mouse and human pancreatic acinar cells[3].

In Vivo

GSK-7975A inhibits local and systemic features of acute pancreatitis in TLCS-AP, CER-AP, FAEE-AP, in dose- and time-dependent manners. GSK-7975A significantly reduces increases in serum amylase, IL6, and pancreatic MPO levels; lung MPO is reduced significantly by low dose only. GSK-7975A markedly reduces pancreatic histopathology in TLCS-AP, CER-AP, and FAEE-AP[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 90 mg/mL (226.53 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5170 mL 12.5849 mL 25.1699 mL
5 mM 0.5034 mL 2.5170 mL 5.0340 mL
10 mM 0.2517 mL 1.2585 mL 2.5170 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[3]

Mice: Acute pancreatitis is induced in C57BL/6J mice by ductal injection of taurolithocholic acid 3-sulfate or intravenous' administration of cerulein or ethanol and palmitoleic acid. Some mice then are given GSK-7975A, which inhibit ORAI1, at different time points to assess local and systemic effects. Sampling of GSK-7975A is at 1, 2, 4, 10, and 22 hours after osmotic minipump insertion from 3 mice/time point. Immediately after humane killing, blood is collected into a heparinized tube, diluted 1:1 with sterile water, and the pancreas is removed and homogenized. Standards and study samples (50 μL from blood and 100 μL from pancreas) are extracted by protein precipitation and centrifuged. Supernatants are dried under heated nitrogen (40°C). Levels of GSK-7975A and GSK-6288B are determined[3].

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

References
Molecular Weight

397.30

Formula

C₁₈H₁₂F₅N₃O₂

CAS No.

1253186-56-9

SMILES

O=C(NC1=NN(CC2=CC=C(O)C=C2C(F)(F)F)C=C1)C3=C(F)C=CC=C3F

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.56%

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Product Name:
GSK-7975A
Cat. No.:
HY-12507
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GSK-7975A

Cat. No.: HY-12507