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(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $151 | In Stock | In Stock | |
| 5 mg | $298 | In Stock | In Stock | |
| 10 mg | $433 | In Stock | In Stock | |
| 25 mg | $678 | In Stock | In Stock | |
| 50 mg | $912 | In Stock | In Stock | |
| 100 mg | $1,180 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $389 | In Stock | In Stock |
| Description | (±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. |
| In vitro | Tazifylline potently inhibits histamine H1-receptor-induced contractions in isolated guinea pig ilea and demonstrates high affinity in radioligand binding studies[1]. |
| In vivo | In anesthetized guinea pigs, Tazifylline causes an inhibition in histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline reduces the inflammatory effects of intradermal histamine. In conscious dogs, Tazifylline(orally) causes inhibition in histamine-induced skin inflammation for long periods of time, and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1 receptors. Large oral doses of Tazifylline do not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats[1]. |
| Molecular Weight | 472.6 |
| Formula | C23H32N6O3S |
| Cas No. | 79712-55-3 |
| Smiles | C(C(CN1CCN(CCCSC2=CC=CC=C2)CC1)O)N3C4=C(N=C3)N(C)C(=O)N(C)C4=O |
| Relative Density. | 1.34g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (95.22 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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