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Pranlukast hemihydrate

Cat. No. M7995
Pranlukast hemihydrate Structure
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Quality Control & Documentation
Biological Activity

Pranlukast is a subtype specific CysLT1 receptor antagonist. Leukotrienes are involved in the inflammation response and are divided into two main classes; leukotriene B4 and cysteinyl-substituted leukotrienes.

Chemical Information
Molecular Weight 490.51
Formula C27H23N5O4 · 0.5 H2O
CAS Number 150821-03-7
Solubility (25°C) DMSO: ≥10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Hiromasa Uchiyama, et al. A simple blending with α-glycosylated naringin produces enhanced solubility and absorption of pranlukast hemihydrate

[2] Eun-Sol Ha, et al. Improving dissolution and oral bioavailability of pranlukast hemihydrate by particle surface modification with surfactants and homogenization

[3] Hideaki Furuta, et al. Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs I: anhydrates and hydrate

[4] Myoung-Ki Baek, et al. Self-microemulsifying drug-delivery system for improved oral bioavailability of pranlukast hemihydrate: preparation and evaluation

[5] Hiromasa Uchiyama, et al. α-Glucosyl hesperidin induced an improvement in the bioavailability of pranlukast hemihydrate using high-pressure homogenization

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