Product Name :
A-740003
Description:
A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.
CAS:
861393-28-4
Molecular Weight:
474.55
Formula:
C26H30N6O3
Chemical Name:
N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide
Smiles :
CC(C)(C)C(NC(=O)CC1C=C(OC)C(=CC=1)OC)/N=C(/NC#N)\NC1=CC=CC2=NC=CC=C21
InChiKey:
PUHSRMSFDASMAE-UHFFFAOYSA-N
InChi :
InChI=1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.|Product information|CAS Number: 861393-28-4|Molecular Weight: 474.55|Formula: C26H30N6O3|Synonym:|A 740003|A740003|Chemical Name: N-[1-[[(Cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxybenzeneacetamide|Smiles: CC(C)(C)C(NC(=O)CC1C=C(OC)C(=CC=1)OC)/N=C(/NC#N)\NC1=CC=CC2=NC=CC=C21|InChiKey: PUHSRMSFDASMAE-UHFFFAOYSA-N|InChi: InChI=1S/C26H30N6O3/c1-26(2,3)24(31-23(33)15-17-11-12-21(34-4)22(14-17)35-5)32-25(29-16-27)30-20-10-6-9-19-18(20)8-7-13-28-19/h6-14,24H,15H2,1-5H3,(H,31,33)(H2,29,30,32)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO 95 mg/mL (200.19 mM) Ethanol 1.5 mg/mL (3.16 mM)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{SHH Protein, Human} web|{SHH Protein, Human} Technical Information|{SHH Protein, Human} In stock|{SHH Protein, Human} custom synthesis|{SHH Protein, Human} Autophagy} |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|A 438079 or A 740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response.{{Besifovir} MedChemExpress|{Besifovir} Anti-infection|{Besifovir} Technical Information|{Besifovir} References|{Besifovir} manufacturer|{Besifovir} Cancer} A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells.PMID:25046520 A-740003 infusions increases SE-induced neuronal death. A-740003 and A-438079 show significantly greater potency in blocking P2X7 receptor activation across all species compared with other antagonists. A-740003 and A-438079 show greater activity at rat and human, as compared with mouse P2X7 receptors. A-740003 potently blocks agonist-evoked IL-1β release with (IC50=156 nM) and pore formation (IC50=92 nM) in differentiated human THP-1 cells.|In Vivo:|Systemic administration of A-740003 produces dose-dependent antinociception in a spinal nerve ligation model (ED50=19 mg/kg i.p.) in the rat. A-740003 also attenuates tactile allodynia in two other models of neuropathic pain, chronic constriction injury of the sciatic nerve and vincristine-induced neuropathy. In addition, A-740003 effectively reduces thermal hyperalgesia observed following intraplantar administration of carrageenan or complete Freund’s adjuvant (ED50=38-54 mg/kg i.p.). A-740003 is ineffective in attenuating acute thermal nociception in normal rats and does not alter motor performance at analgesic doses.|References:|Prisca Honore, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):Grol MW, et al. P2X?-mediated calcium influx triggers a sustained, PI3K-dependent increase in metabolic acid production by osteoblast-like cells. Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E561-75.Honore P, et al. A-740003 [N-(1-{[(cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a novel and selective P2X7 receptor antagonist, dose-dependently reduces neuropathic pain in the rat. J Pharmacol Exp Ther. 2006 Dec;319(3):1376-85. Epub 2006 Sep 18.Products are for research use only. Not for human use.|
