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. 2018 Feb 28;132(4):489–507. doi: 10.1042/CS20180031

Table 2. Key pharmacological properties of linagliptin and other globally marketed DPP-4 inhibitors.

Compound IC50 (nM) [134] KD (nM) [134] kon (M−1.s−1) [134] koff × 10−4 (s−1) [134] VD [20] Renal excretion (%) [20] Protein binding (%) [20]
Alogliptin 35.5 2.4 1.3 × 106 31 581 63.3 20
Linagliptin 1.4 0.0066 7.6 × 106 0.51 1110−3060 6.3 75−99
Saxagliptin 55.0 0.3 9.2 × 105 2.0 151 24 <10
Sitagliptin 45.0 5.3 1.5 × 107 630 198 75 38
Vildagliptin 95.5 2.4 7.1 × 104 1.7 70.5 22.6 9

Abbreviations: KD, equilibrium dissociation constant; kon, rate constant for association of the DPP-4/inhibitor complex; koff, rate constant for dissociation of the DPP-4/inhibitor complex; VD, volume of distribution.