GSK2982772 [1622848-92-3]
Cat# HY-101760-10mg
Size : 10mg
Brand : MedChemExpress
GSK2982772 est un inhibiteur de kinase de RIP1 qui est puissant, oralement actif et compétitif avec l'ATP, avec des valeurs IC50 de 16 nM et 20 nM pour le RIP1 humain et singe, respectivement.
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.
For research use only. We do not sell to patients.
GSK2982772 Chemical Structure
CAS No. : 1622848-92-3
This product is a controlled substance and not for sale in your territory.
Based on 2 publication(s) in Google Scholar
Description |
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively[1]. |
IC50 & Target |
IC50: 16 nM (human RIP1 FP)IC50: 20 nM (monkey RIP1 FP)IC50: 2 μM (rat RIP1 FP)IC50: 2.5 μM (mouse RIP1 FP)[1] |
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In Vitro |
GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases at 10 μM. In stimulated cellular systems,GSK2982772 is also able to reduce spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue in overnight incubations. GSK2982772 produces a weak concentration dependent inhibition of hERG in human embryonic kidney (HEK-293) cells, with an estimated IC50 of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC50 of 13 μM[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10-6 cm/s)[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
377.40 |
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Formula |
C20H19N5O3 |
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CAS No. |
1622848-92-3 |
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Appearance |
Solid |
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Color |
White to yellow |
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SMILES |
O=C(C1=NC(CC2=CC=CC=C2)=NN1)N[C@H]3COC4=CC=CC=C4N(C)C3=O |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 250 mg/mL (662.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : < 0.1 mg/mL (insoluble) Preparing
Stock Solutions
View the 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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Purity & Documentation |
Purity: 98.98% |
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References |
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.6497 mL | 13.2485 mL | 26.4971 mL | 66.2427 mL |
5 mM | 0.5299 mL | 2.6497 mL | 5.2994 mL | 13.2485 mL | |
10 mM | 0.2650 mL | 1.3249 mL | 2.6497 mL | 6.6243 mL | |
15 mM | 0.1766 mL | 0.8832 mL | 1.7665 mL | 4.4162 mL | |
20 mM | 0.1325 mL | 0.6624 mL | 1.3249 mL | 3.3121 mL | |
25 mM | 0.1060 mL | 0.5299 mL | 1.0599 mL | 2.6497 mL | |
30 mM | 0.0883 mL | 0.4416 mL | 0.8832 mL | 2.2081 mL | |
40 mM | 0.0662 mL | 0.3312 mL | 0.6624 mL | 1.6561 mL | |
50 mM | 0.0530 mL | 0.2650 mL | 0.5299 mL | 1.3249 mL | |
60 mM | 0.0442 mL | 0.2208 mL | 0.4416 mL | 1.1040 mL | |
80 mM | 0.0331 mL | 0.1656 mL | 0.3312 mL | 0.8280 mL | |
100 mM | 0.0265 mL | 0.1325 mL | 0.2650 mL | 0.6624 mL |