TC-P 262Selective P2X3, P2X2/3 antagonist CAS# 873398-67-5 |
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Quality Control & MSDS
3D structure
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| Cas No. | 873398-67-5 | SDF | Download SDF |
| PubChem ID | 59598765 | Appearance | Powder |
| Formula | C14H18N4O | M.Wt | 258.32 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in DMSO | ||
| Chemical Name | 5-(5-methyl-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine | ||
| SMILES | CC1=CC(=C(C=C1)C(C)C)OC2=CN=C(N=C2N)N | ||
| Standard InChIKey | RAKSAPLZNJXYRB-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C14H18N4O/c1-8(2)10-5-4-9(3)6-11(10)19-12-7-17-14(16)18-13(12)15/h4-8H,1-3H3,(H4,15,16,17,18) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective P2X3 and P2X2/3 receptor antagonist (pIC50 values are 7.39 and 6.68 respectively). Displays no detectable activity at P2X1, P2X2, P2X4 and P2X7 receptors (pIC50 < 4.7). |
TC-P 262 Dilution Calculator
TC-P 262 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.8712 mL | 19.3558 mL | 38.7117 mL | 77.4234 mL | 96.7792 mL |
| 5 mM | 0.7742 mL | 3.8712 mL | 7.7423 mL | 15.4847 mL | 19.3558 mL |
| 10 mM | 0.3871 mL | 1.9356 mL | 3.8712 mL | 7.7423 mL | 9.6779 mL |
| 50 mM | 0.0774 mL | 0.3871 mL | 0.7742 mL | 1.5485 mL | 1.9356 mL |
| 100 mM | 0.0387 mL | 0.1936 mL | 0.3871 mL | 0.7742 mL | 0.9678 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Characterization of three diaminopyrimidines as potent and selective antagonists of P2X3 and P2X2/3 receptors with in vivo efficacy in a pain model.[Pubmed:21410458]
Br J Pharmacol. 2011 Jul;163(6):1315-25.
BACKGROUND AND PURPOSE: P2X3 and P2X2/3 receptors are highly localized on the peripheral and central pathways of nociceptive signal transmission. The discovery of A-317491 allowed their validation as chronic inflammatory and neuropathic pain targets, but this molecule has a very limited oral bioavailability and CNS penetration. Recently, potent P2X3 and P2X2/3 blockers with a diaminopyrimidine core group and better bioavailability were synthesized and represent a new opportunity for the validation of P2X3-containing receptors as targets for pain. Here we present a characterization of three representative diaminopyrimidines. EXPERIMENTAL APPROACH: The activity of compounds was evaluated in intracellular calcium flux and electrophysiological recordings from P2X receptors expressed in mammalian cells and in a in vivo model of inflammatory pain (complete Freund's adjuvant (CFA) in rat paws). KEY RESULTS: Compound A potently blocked P2X3 (pIC(50)= 7.39) and P2X2/3 (pIC(50)=6.68) and showed no detectable activity at P2X1, P2X2, P2X4 and P2X7 receptors (pIC(50)< 4.7). Whole-cell voltage clamp electrophysiology confirmed these results. Compounds showed good selectivities when tested against a panel of different classes of target. In the CFA model, compound B showed significant anti-nociceptive effects (57% reversal at 3mg.kg(-1) ). CONCLUSIONS AND IMPLICATIONS: The diaminopyrimidines were potent and selective P2X3 and P2X2/3 receptor antagonists, showing efficacy in vivo and represent useful tools to validate these receptors as targets for inflammatory and neuropathic pain and provide promising progress in the identification of therapeutic tools for the treatment of pain-related disorders.
