Aprepitant

Product Description

Aprepitant is a potent long-acting hNK-1 antagonist (IC₅₀ = 0.09 nM and K_d = 19 pM) that inhibits the effect of substance P on NK-1 receptors. Inhibits metastasis and impairs tumor growth in patient derived xenografts and breast cancer cells. In an animal model of intracerebral hemorrhage, Aprepitant reduces neurological impairment, neuronal damage and neuronal death. Suppresses pain and inflammation induced by formalin. Inhibits induced foot-tapping in gerbils. CNS penetrant and orally bioavailable. Antiemetic.

Solubility

Preparing Stock Solutions for Aprepitant

The following data is based on the product molecular weight 534.43

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.87 mL	9.36 mL	18.71 mL
5 mM	0.37 mL	1.87 mL	3.74 mL
10 mM	0.19 mL	0.94 mL	1.87 mL
50 mM	0.04 mL	0.19 mL	0.37 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Yang Aprepitant inhibits JNK and p38/MAPK to attenuate inflammation and suppresses inflammatory pain. Front.Pharmacol. 2022 PMID: 35087409
• Jin Aprepitant attenuates NLRC4-dependent neuronal pyroptosis via NK1R/PKCd pathway in a mouse model of intracerebral hemorrhage. J.Neuroinflammation 2022 PMID: 35922848
• Padmanaban Neuronal substance P drives metastasis through an extracellular RNA-TLR7 axis. Nature 2024 PMID: 39112700
• Hale Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 recepto J.Med.Chem. 1998 PMID: 9804700