15-Deoxy-TIC
15-Deoxy-TIC is a selective central nervous system-type prostacyclin receptor (IP2) ligand that can cross the blood-brain barrier. 15-Deoxy-TIC binds to IP2 with a rat IC50 of 3 nM, activates the cAMP/PKA signaling pathway, and inhibits CXCL9/CXCL10. 15-Deoxy-TIC inhibits oxidative stress/trophic factor withdrawal-induced neuronal apoptosis. 15-Deoxy-TIC can be used for research on focal cerebral ischemia, central nervous system neuronal injury, and neurodegenerative diseases.
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- CAS No.: 220119-27-7
- Formule: C24H32O3
- Masse moléculaire:368.51
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
|
IP2 3 nM (IC50) |
cAMP |
PKA |
CXCL9 |
CXCL10 |
In Vitro
15-Deoxy-TIC-mediated chemokine inhibition in BEAS-2B cells is competitively antagonized by RO3244794 (HY-164580), with pKb values of 9.90 and 9.79 for CXCL9 and CXCL10, respectively[2].
Inhibition of CXCL9 and CXCL10 release from BEAS-2B cells by 15-Deoxy-TIC requires cAMP/PKA signaling, as PKA inhibition blocks this response[2].
15-Deoxy-TIC binds to CNS-type IP2 receptors with an IC50 of 3 nM and to IP1 receptors with an IC50 of 1 μM in frozen tissue sections containing the thalamus and NTS[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongolian gerbils, weigh-ing 60-80 g[4]
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Dosage:0.5-10 µM in the minipump; 100 µM (brain temperature)
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Administration:i.c.v.; continuous infusion at approximately 1 µL/h; starting 2 days before ischemia
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Result:Continuous i.c.v. infusion rescued CA1 pyramidal neurons from ischemia-induced death in a dose-dependent manner at 0.5-10 µM in the minipump.
At 10 µM, rescued almost all CA1 pyramidal neurons in this ischemic model.
At concentrations greater than 100 µM, the neuroprotective effect diminished.
In the brain-temperature cohort, continuous infusion at 100 µM (n = 4) did not significantly reduce brain temperature.
Chemical Information
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CAS No. 220119-27-7
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Masse moléculaire 368.51
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Formule C24H32O3
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SMILES
CC1=CC=CC(CC/C=C/[C@@H]2[C@]3([H])[C@@](C[C@H]2O)([H])C=C(C3)CCCCC(O)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Takamatsu H, et al. Specific ligand for a central type prostacyclin receptor attenuates neuronal damage in a rat model of focal cerebral ischemia. Brain research. 2002 Jan 25;925(2):176-82. [Content Brief]
[2]. Wilson SM, et al. Evidence for a second receptor for prostacyclin on human airway epithelial cells that mediates inhibition of CXCL9 and CXCL10 release. Molecular pharmacology. 2011 Mar 1;79(3):586-95. [Content Brief]
[4]. Cui Y, et al. Protective effect of prostaglandin I2 analogs on ischemic delayed neuronal damage in gerbils. Biochemical and biophysical research communications. 1999 Nov 19;265(2):301-4. [Content Brief]
[5]. Satoh T, et al. CNS-specific prostacyclin ligands as neuronal survival-promoting factors in the brain. The European journal of neuroscience. 1999 Sep;11(9):3115-24. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
15-Deoxy-TIC Related Classifications
HY-189088 Related Classifications
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Keywords
- 15-Deoxy-TIC
- 220119-27-7
- Prostaglandin Receptor
- PKA
- CXCR
- Apoptosis
- Protein kinase A
- CXC chemokine receptors
- C-X-C motif chemokine receptors
- CXCL10
- CXCL9
- IP1 receptor
- IP2 receptor
- cAMP/PKA signaling
- focal cerebral ischemia
- neurodegeneration
- neuronal apoptosis
- oxidative stress
- prostacyclin receptor
- Inhibitor
- inhibitor
- inhibit