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Cat. No.: HY-101601

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Bamirastine

Name: Bamirastine
Brand: MedChemExpress
SKU: HY-101601
Price: 1347.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: TAK-427)

Bamirastine inhibits ligand binding to recombinant human histamine H₁ receptors (rhH₁R) with an IC₅₀ value of 17.3 nM.

For research use only. We do not sell to patients.

CAS No.: 215529-47-8
Formula: C₃₁H₃₇N₅O₃
Molecular Weight:527.66

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

Bamirastine Chemical Structure

CAS No.: 215529-47-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Bamirastine inhibits ligand binding to recombinant human histamine H₁ receptors (rhH₁R) with an IC₅₀ value of 17.3 nM.

IC₅₀ & Target

IC50: 17.3 nM (rhH₁R)^[1]

All Histamine Receptor Isoforms :

In Vitro

Bamirastine (TAK-427) reduces specific binding of [³H] pyrilamine to recombinant human H₁ receptors (rhH₁R) is seen in a concentration- dependent manner with an IC₅₀ value of 17.3 nM. The K_i value is calculated to be 7.35 nM. The affinity of Bamirastine is found to be as high as that of azelastine, 2 times lower than that of Epinastine, 8 times lower than that of ketotifen and 3 times higher than that of Terfenadine^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

Bamirastine (TAK-427) inhibits histamine induced skin reactions in guinea pigs and mice with an ID₅₀ value of 0.884 and 0.450 mg/kg, p.o., respectively; significant inhibition associated with 10 mg/kg of Bamirastine is still observed 24 h after dosing in guinea pigs. Even at 300 mg/kg, Bamirastine does not affect pentobarbital-induced sleeping time in mice. Bamirastine significantly inhibits passive cutaneous anaphylaxis (PCA) in mice and guinea pigs, and also inhibits antigen-induced ISRs in guinea pigs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 215529-47-8
Molecular Weight 527.66
Formula C₃₁H₃₇N₅O₃
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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