GSK2220691
Based on 1 publication(s) in Google Scholar
GSK2220691 is a TRPV4 inhibitor. GSK2220691 inhibits agonist-induced calcium influx and downstream vascular leakage, and has anti-inflammatory effects, reducing neutrophil/macrophage infiltration, pro-inflammatory cytokines/chemokines, protein leakage, vascular injury markers, and blood oxygen desaturation, while protecting pulmonary and systemic vascular barrier function. GSK2220691 can be used in research on acute lung injury and phosgene-induced acute respiratory distress syndrome (ARDS).
For research use only. We do not sell to patients.
- Purity : 99.96%
- CAS No.: 1206619-37-5
- Formula: C32H33N5O3
- Molecular Weight:535.64
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK2220691
More
Biological Activity
Description
|
TRPV4 |
In Vitro
GSK2220691 shows IC50 <4.6 nM (n = 2-6) against TRPV1, TRPA1, TRPC3, TRPC6, TRPM5, and TRPM8 in FLIPR selectivity assays, with TRPA1, TRPC3, TRPC6, and TRPM5 EC50 <4.6 nM as reported[1].
GSK2220691 inhibits agonist-induced calcium influx in human TRPV4-transfected HEK293T cells with an IC50 of 50.5 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GSK2220691 (15-30 mg/kg; intraperitoneal or intramuscular; immediately after Cl2 exposure and 8 h after beginning exposure) protects against chlorine-induced airway hyperreactivity, edema, inflammation, vascular damage, oxygen desaturation, and histopathological lung injury in mice[1].
GSK2220691 (30 mg/kg; i.p.; single administration at 30 minutes post-phosgene exposure) attenuates phosgene-induced acute lung injury in male BALB/c mice by reducing body weight loss, BALF protein/albumin/leukocyte increases, and pro-inflammatory cytokine transcript/protein levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (male, 8-10 weeks old, 20-25 g body weight)[1]
-
Dosage:30 mg/kg body weight
-
Administration:intraperitoneal; single; 30 min after HCl instillation
-
Result:BALF neutrophils and macrophages were reduced and MPO activity decreased in HCl-exposed mice.
Histopathological lung injury scores were strongly reduced.
HCl-induced increases in BALF VEGF, KC (CXCL1), and G-CSF were completely suppressed.
Serum markers of pulmonary injury (IL-6, KC, G-CSF) were reduced to almost baseline levels.
-
Animal Model:C57BL/6 (male, 8-10 weeks old, 20-25 g body weight)[1]
-
Dosage:30 mg/kg body weight immediately after Cl2 exposure, then 15 mg/kg body weight at 8 h post-exposure
-
Administration:intraperitoneal or intramuscular; immediately after Cl2 exposure and 8 h after beginning exposure
-
Result:In Cl2-exposed mice, airway reactivity to Methacholine remained at baseline levels and lung elastance was strongly reduced.
Blood oxygen saturation remained at baseline equivalent to uninjured mice breathing air.
BALF protein content was strongly reduced.
BALF macrophage and neutrophil counts were reduced to almost baseline, and MPO activity was reduced.
Increases in BALF KC (CXCL1), G-CSF, and VEGF were strongly suppressed to levels near baseline.
Serum increases in KC, G-CSF, and IL-6 were reduced.
BALF vascular damage markers SAP, fibrinogen, adiponectin, and sVCAM-1 were strongly reduced.
Histopathological analysis showed reduced histopathological lung injury in representative sections compared with chlorine-exposed controls.
-
Animal Model:BALB/c (male, 8-9 weeks old, 20-30 g)[2]
-
Dosage:30 mg/kg
-
Administration:i.p.; single administration at 30 minutes post-phosgene exposure
-
Result:Reduced post-phosgene body weight loss, decreased BALF albumin and total protein, and reduced recruitment of BALF total leukocytes compared with vehicle-treated mice.
Significantly reduced lung transcript levels of IL-6, KC, and MIP-2, and reduced protein levels of TNFα, MIP-2, and MMP9.
Chemical Information
-
CAS No. 1206619-37-5
-
Appearance Solid
-
Molecular Weight 535.64
-
Formula C32H33N5O3
-
Color White to off-white
-
SMILES
O=C(N[C@@H](C(C)(C)C)C(N1[C@](C2)([H])CN(C(C3=CC=C(C4=CC=CC=C4)C=N3)=O)[C@]2([H])C1)=O)C5=CC6=C(N5)C=CC=C6
-
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
Publications (1)
-
Journal Impact Factor
-
Most Recent
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (186.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (290 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8669 mL | 9.3346 mL | 18.6693 mL | 46.6731 mL |
| 5 mM | 0.3734 mL | 1.8669 mL | 3.7339 mL | 9.3346 mL | |
| 10 mM | 0.1867 mL | 0.9335 mL | 1.8669 mL | 4.6673 mL | |
| 15 mM | 0.1245 mL | 0.6223 mL | 1.2446 mL | 3.1115 mL | |
| 20 mM | 0.0933 mL | 0.4667 mL | 0.9335 mL | 2.3337 mL | |
| 25 mM | 0.0747 mL | 0.3734 mL | 0.7468 mL | 1.8669 mL | |
| 30 mM | 0.0622 mL | 0.3112 mL | 0.6223 mL | 1.5558 mL | |
| 40 mM | 0.0467 mL | 0.2334 mL | 0.4667 mL | 1.1668 mL | |
| 50 mM | 0.0373 mL | 0.1867 mL | 0.3734 mL | 0.9335 mL | |
| 60 mM | 0.0311 mL | 0.1556 mL | 0.3112 mL | 0.7779 mL | |
| 80 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5834 mL | |
| 100 mM | 0.0187 mL | 0.0933 mL | 0.1867 mL | 0.4667 mL |
GSK2220691 Related Classifications
HY-176464 Related Classifications
Powered by Bioz
Keywords
- GSK2220691
- 1206619-37-5
- GSK 2220691
- GSK-2220691
- TRP Channel
- ARDS
- BALB/c mice
- HEK293 cells
- HEK293T cells
- TRPA1
- TRPC3
- TRPC6
- TRPM5
- TRPM8
- TRPV1
- TRPV4
- acute lung injury
- acute respiratory distress syndrome
- airway mechanics
- anti-inflammatory
- arterial blood pressure
- calcium influx
- chemokines
- chlorine-induced airway hyperreactivity
- dogs
- hypotension
- lung elastance
- macrophage infiltration
- mice
- monkeys
- neutrophil infiltration
- phosgene-induced pulmonary injury
- proinflammatory cytokines
- pulmonary edema
- pulmonary inflammation
- rats
- vascular barrier function
- vascular leakage
- Inhibitor
- inhibitor
- inhibit