- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. ] A-317491sodiumsalthydrate
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15568A |
| Brand: | MCE |
| CAS: | - |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 606.57 |
| Molecular Formula | C33H29NNaO9 |
| SMILES | O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O.[Na].O |
3 Publications Citing Use of MCE
Summary
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X 3 and P2X 2/3 receptors , with K i s of 22, 22, 9, and 92 nM for hP2X 3 , rP2X 3 , hP2X 2/3 , and rP2X 2/3 , respectively. A-317491 sodium salt hydrate is highly selective ( IC50 >10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X 3 and P2X 2/3 receptor-mediated calcium flux [1] [2] .
IC50 & Target
Ki: 22 nM (hP2X3), 22 nM (rP2X3), 9 nM (hP2X2/3), 92 nM (rP2X2/3) [1]
In Vitro
A-317491 potently blocks recombinant human and rat P2X
3
and P2X
2/3
receptor-mediated calcium flux (K
i
=22-92 nM)
[1]
.
A-317491 (1 nM-10 μM) produces a concentration-dependent block of dorsal root ganglion (DRG) currents with an IC
50
of 15 nM
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
A-317491 (0.1-30 mg/kg; a single s.c.) dose-dependently reverses inflammatory mechanical hyperalgesia in rats
[2]
.
A-317491 (3-30 mg/kg; a single .v.) exhibits the plasma half-life (7.38 h), clearance rate (1.83 L/h/kg), and volume of distribution (0.17 L/kg)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male adult Sprague-Dawley rats received an intraplantar injection of Freund's complete adjuvant [2] |
| Dosage: | 0.1, 1, 3, 10, 30 mg/kg |
| Administration: | A single s.c. |
| Result: | Produced a dose-dependent reduction in mechanical hyperalgesia 1 h, 3 h and 5 h post-administration. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 164.86 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6486 mL | 8.2431 mL | 16.4861 mL |
| 5 mM | 0.3297 mL | 1.6486 mL | 3.2972 mL |
| 10 mM | 0.1649 mL | 0.8243 mL | 1.6486 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (82.43 mM); Clear solution; Need ultrasonic
References
- [1] Jarvis MF, et, al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84.
- [2] Wu G, et, al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53.
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.