p38α inhibitor 4

Cat. No. M42150

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Quality Control & Documentation

Purity:
COA
MSDS

Product Information

Biological Activity

p38α inhibitor 4 is a selective and allosteric p38α inhibitor with an IC50 value of 1.2 μM.

Chemical Information

Molecular Weight	347.22
Formula	C14H7F6N3O
CAS Number	1262406-08-5
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
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tomoyuki Hashimoto et al. Ann Nucl Med. Radiobrominated probe targeting activated p38α in inflammatory diseases

[2] Rania Khalil et al. Toxicol Appl Pharmacol. Vildagliptin, a DPP-4 inhibitor, attenuates carbon tetrachloride-induced liver fibrosis by targeting ERK1/2, p38α, and NF-κB signaling

[3] Wolfgang Albrecht et al. J Med Chem. Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases

[4] Chunjian Liu et al. J Med Chem. Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor

[5] Amit S Kalgutkar et al. Biopharm Drug Dispos. Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes

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Signaling Pathways

p38α inhibitor 4

Quality Control & Documentation

Biological Activity

Chemical Information

Conversion of different model animals based on BSA (PMID: 27057123)

References

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