A-740003

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A-740003 is a selective and competitive antagonist of P2X7 receptor with IC50 values of 40 nM and 18 nM in human and rat, respectively [1].
P2X7 receptors are members of ATP-sensitive ionotropic P2X receptor family (P2X1–P2X7). P2X7 receptors can trigger various responses such as activation of caspases, cytokine release, membrane permeabilization, apoptosis and cell proliferation, in immunologically genetic cells [1].
Activated P2X7 receptors rapidly change intracellular calcium concentrations, the release of interleukin-1β (IL-1β), and cytolytic plasma membrane pore formation. In human THP-1 cells with a macrophage phenotype that P2X7 receptors were expressed, IL-1β release and pore formation were resulted from the activation of P2X7 receptors. A-740003 potently inhibited pore formation (measured by Yo-Pro uptake) with an IC50 value of 92 nM and blocked the release of IL-1β with an IC50 value of 156 nM [1].
Homomeric P2X7 receptors were activated by 2´,3´-O-(4-benzoylbenzoyl)-ATP (BzATP) and ATP at high concentrations. This property made homomeric P2X7 receptors different from other P2 receptor superfamily members. In 1321N1 cells stably expressing P2X7 receptors, BzATP changed intracellular calcium concentrations. A-740003 potently inhibited this change with an IC50 value of 18 nM when rat P2X7 receptors were expressed, and an IC50 value of 40 nM when human P2X7 receptors were expressed. A-740003 also inhibited intracellular Yo-Pro uptake with IC50 values of 138 nM and 93 nM, when the Yo-Pro uptake was mediated by rat and human P2X7 receptors, respectively [1].
Reference:
[1]. Prisca Honore, Diana Donnelly-Roberts, Marian T. Namovic, 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. Journal of Pharmacology and Experimental Therapeutics, 2006, 319:1376-1385.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 474.57 |
Cas No. | 861393-28-4 |
Formula | C26H30N6O3 |
Synonyms | A 740003;A740003 |
Solubility | ≥23.73 mg/mL in DMSO; insoluble in H2O; ≥2.48 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | N-[1-[(E)-[(cyanoamino)-(quinolin-5-ylamino)methylidene]amino]-2,2-dimethylpropyl]-2-(3,4-dimethoxyphenyl)acetamide |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C(NC(=O)CC1=CC(=C(C=C1)OC)OC)N=C(NC#N)NC2=CC=CC3=C2C=CC=N3 |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Description | A-740003 is potent, selective and competitive antagonist of P2X7 receptor with IC50 values of 18 nM and 40 nM for rat and human receptors, respectively. | |||||
Targets | P2X7 receptor | |||||
IC50 | 18 nM (rat) 40 nM (human) |
Quality Control & MSDS
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Chemical structure
