Size | Price | |
---|---|---|
10mg | ||
25mg | ||
50mg | ||
100mg | ||
250mg |
Purity: ≥98%
Bamirastine (also known as TAK-427),a new imidazopyridazine derivative, is a novelantihistamine compound withantiallergic effects. It inhibits ligand binding to recombinant human histamine H1receptors (rhH1R) with anIC50value of 17.3 nM.TAK-427 inhibited ligand binding to rhH(1)R with an IC(50) value of 17.3 nmol/l. TAK-427 inhibited histamine-induced skin reactions in guinea pigs and mice with an ID(50) value of 0.884 and 0.450 mg/kg, p.o., respectively; significant inhibition associated with 10 mg/kg of TAK-427 was still observed 24 h after dosing in guinea pigs. TAK-427 showed as high selectivity for peripheral H(1) receptors as terfenadine and epinastine did, which was evaluated by ex vivo measured radioligand binding. Even at 300 mg/kg, TAK-427 did not affect pentobarbital-induced sleeping time in mice. TAK-427 significantly inhibited PCA in mice and guinea pigs, and also inhibited antigen-induced ISRs in guinea pigs.
ln Vitro |
Bamirastine (TAK-427) has an IC50 value of 17.3 nM and decreases the concentration-dependent specific binding of [3H]pyrilamine to recombinant human H1 receptor (rhH1R). A value of 7.35 nM was determined for the Ki. Based on research, bamistin's affinity is 3 times higher than fenadine, 2 times lower than epinastine, 8 times lower than ketotifen, and as high as azelastine [1].
|
---|---|
ln Vivo |
In guinea pigs and mice, bamirastine (TAK-427) inhibits histamine-induced skin reactions with ID50 values of 0.884 and 0.450 mg/kg, respectively, when administered orally; 24 hours after dosing, in guinea pigs, the same effects as 10 mg/kg Bamirastine were still observed in guinea pigs Stine-related significant inhibition. In mice, even at 300 mg/kg, bamistin had no effect on the length of pentobarbital-induced drowsiness. Bamistin clearly suppresses antigen-induced immunological response (ISR) in guinea pigs and mice, as well as the passive cutaneous allergic response (PCA) in mice [1].
|
References |
[1]. Fukuda S, et al. Characteristics of the antihistamine effect of TAK-427, a novel imidazopyridazine derivative. Inflamm Res. 2003 May;52(5):206-14
|
Molecular Formula |
C31H37N5O3
|
---|---|
Molecular Weight |
527.6572
|
CAS # |
215529-47-8
|
SMILES |
O=C(O)C(C)(C)C1=CN2N=C(NCCCN3CCC(OC(C4=CC=CC=C4)C5=CC=CC=C5)CC3)C=CC2=N1
|
Synonyms |
TAK-427; TAK 427; TAK427
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8952 mL | 9.4758 mL | 18.9516 mL | |
5 mM | 0.3790 mL | 1.8952 mL | 3.7903 mL | |
10 mM | 0.1895 mL | 0.9476 mL | 1.8952 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.