A-740003 structure
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Common Name | A-740003 | ||
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CAS Number | 861393-28-4 | Molecular Weight | 474.555 | |
Density | 1.2±0.1 g/cm3 | Boiling Point | N/A | |
Molecular Formula | C26H30N6O3 | Melting Point | N/A | |
MSDS | Chinese USA | Flash Point | N/A | |
Symbol |
GHS06 |
Signal Word | Danger |
Use of A-740003A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively. |
Name | N-[1-[(E)-[(cyanoamino)-(quinolin-5-ylamino)methylidene]amino]-2,2-dimethylpropyl]-2-(3,4-dimethoxyphenyl)acetamide |
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Synonym | More Synonyms |
Description | A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively. |
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Related Catalog | |
Target |
IC50: 18 nM (rat P2X7 receptor), 40 nM (human P2X7 receptor) |
In Vitro | A 438079 or A 740003 (10 μM) significantly blocks the sustained phase of the BzATP-induced response[1]. A-740003 infusion reduces SE-induced TNF-α expression in dentate granule cells. A-740003 infusions increases SE-induced neuronal death[2]. 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[3]. 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[4]. |
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[4]. |
Animal Admin | The response to acute thermal stimulation is determined using a commercially available paw thermal stimulator. Rats are placed individually in Plexiglas cubicles mounted on a glass surface maintained at 30°C and allowed a 30-min habituation period. A thermal stimulus, in the form of radiant heat emitted from a focused projection bulb, is then applied to the plantar surface of each hind paw. In each test session, each rat is tested in three sequential trials at approximately 5-min intervals. Paw-withdrawal latencies (PWLs) are calculated as the median of the two shortest latencies. An assay cut off is set at 20.5 s. A-740003 is injected i.p. 30 min before testing for acute thermal pain. |
References |
Density | 1.2±0.1 g/cm3 |
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Molecular Formula | C26H30N6O3 |
Molecular Weight | 474.555 |
Exact Mass | 474.237946 |
PSA | 120.66000 |
LogP | 2.77 |
Index of Refraction | 1.597 |
Storage condition | 2-8℃ |
Symbol |
GHS06 |
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Signal Word | Danger |
Hazard Statements | H301 |
Precautionary Statements | P301 + P310 |
RIDADR | UN 2811 6.1 / PGIII |
~% A-740003 CAS#:861393-28-4 |
Literature: Journal of Medicinal Chemistry, , vol. 52, # 10 p. 3366 - 3376 |
Precursor 2 | |
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DownStream 0 |
Disruption in connexin-based communication is associated with intracellular Ca²⁺ signal alterations in astrocytes from Niemann-Pick type C mice.
PLoS ONE 8 , e71361, (2013) Reduced astrocytic gap junctional communication and enhanced hemichannel activity were recently shown to increase astroglial and neuronal vulnerability to neuroinflammation. Moreover, increasing evide... |
N-{1-[N''-Cyano-N'-(quinolin-5-yl)carbamimidamido]-2,2-dimethylpropyl}-2-(3,4-dimethoxyphenyl)acetamide |
N-(1-{(E)-[(Cyanoamino)(5-quinolinylamino)methylene]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide |
cc-516 |
UNII:532OV6WA05 |
Benzeneacetamide, N-[1-[[(1E)-(cyanoamino)(5-quinolinylamino)methylene]amino]-2,2-dimethylpropyl]-3,4-dimethoxy- |
CS-0297 |
A-740003 |