A 740003 is a potent and selective P2X7 receptor antagonist (IC50 values are 18 and 40 nM for rat and human receptors respectively). Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain. Also reduces neuroblastoma tumor growth in mice.
| Molecular Weight | 474.55 |
| Formula | C26H30N6O3 |
| CAS Number | 861393-28-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 9.49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Jie Yin, et al. Role of P2X 7 R in the development and progression of pulmonary hypertension
| Related P2 Receptor Products |
|---|
| Purotoxin 1
Purotoxin 1 is a P2X3 receptor inhibitor. |
| P2X2/3 modulator-1
P2X2/3 modulator-1 is a P2X2/3 modulator. |
| P2X7-IN-2 TFA
P2X7-IN-2 TFA is a P2X7 receptor inhibitor. |
| NP-1815-PX
NP-1815-PX is a potent and selective P2X4R antagonist. |
| P2X3-IN-1
P2X3-IN-1 is an inhibitor of P2X3 receptor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
