GW791343 HCl
目录号 : GC14207GW791343 HCl 是一种有效的人 P2X7 受体负变构调节剂(表现出物种特异性活性),对人 P2X7 受体产生非竞争性拮抗作用,pIC50 为 6.9-7.2。
Cas No.:309712-55-8
Sample solution is provided at 25 µL, 10mM.
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GW791343 3Hcl is a P2X7 allosteric modulator; exhibits species-specific activity and acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2). IC50 value: 7 (pIC50)Target: P2X7 in vitro: In cells expressing human P2X7 receptors, GW 791343 inhibits agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer. In NaCl buffer, GW 791343 reduces the maximal response to both ATP and BzATP, but there is little effect on agonist potency except for a decrease in the presence of 300–1000 nM GW 791343. GW 791343 also reduces maximal responses to ATP and BzATP in sucrose buffer, although this effect is more marked when using ATP as agonist. In sucrose buffer, GW 791343 produces a slight decrease in ATP potency at 300 nM. GW 791343 decreases BzATP potency at concentrations of 300 nM to 10 μM. A more marked increase in agonist effect is observed when using ATP as agonist in NaCl buffer with GW791343 increasing the pEC50 and maximal response to ATP at concentrations of 10 and 30 μM. In sucrose buffer, GW791343 also increases responses when using ATP as agonist [1]. GW791343 inhibits responses at the human–rat chimeric receptor in both sucrose and NaCl buffer. GW791343 increases responses to BzATP at the F95L mutant receptor [2]. GW791343 is a non-competitive antagonist and negative allosteric modulator at the human P2X7 receptor; however, GW 791343 also acts as a positive allosteric modulator at the rat P2X7 receptor [3]. At the dog P2X7 receptor, GW 791343 is an antagonist with similar potency to that determined at the human receptor [4].
References:
[1]. Michel AD, et al. Negative and positive allosteric modulators of the P2X(7) receptor. Br J Pharmacol, 2008, 153(4), 737-750.
[2]. Michel AD, et al. Identification of regions of the P2X(7) receptor that contribute to human and rat species differences in antagonist effects. Br J Pharmacol, 2008, 155(5), 738-751.
[3]. Felix RA, et al. Development of a comprehensive set of P2 receptor pharmacological research compounds. Purinergic Signal, 2012, 8(Suppl 1), 101-112.
[4]. Roman S, et al. Cloning and pharmacological characterization of the dog P2X7 receptor. Br J Pharmacol, 2009, 158(6), 1513-1526.
Cas No. | 309712-55-8 | SDF | |
化学名 | 2-(3,4-difluoroanilino)-N-[2-methyl-5-(piperazin-1-ylmethyl)phenyl]acetamide;trihydrochloride | ||
Canonical SMILES | CC1=C(C=C(C=C1)CN2CCNCC2)NC(=O)CNC3=CC(=C(C=C3)F)F.Cl.Cl.Cl | ||
分子式 | C20H27Cl3F2N4O | 分子量 | 483.81 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.0669 mL | 10.3346 mL | 20.6693 mL |
5 mM | 0.4134 mL | 2.0669 mL | 4.1339 mL |
10 mM | 0.2067 mL | 1.0335 mL | 2.0669 mL |
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