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. 2010 Dec 8;2(2):171–176. doi: 10.1021/ml100251u

Table 4. In Vitro and in Vivo Potencies of 39, 41, and Nicotinic Acid.

  39 41 nicotinic acid
hu-GPR109a EC50 (nM)a 59 ± 56 49 ± 11 100 ± 15
rat-GPR109a EC50 (nM)a 3 ± 1 6 ± 2 39 ± 10
m-GPR109a EC50 (nM)a 4 ± 3 15 ± 5 29 ± 5
dog-GPR109a EC50 (nM)a 21 ± 4 126 ± 58 30 ± 14
cyno-GPR109a (nM)a 2 ± 1 ndb 26 ± 33
hu-GPR109b EC50 (nM)a 300 ± 105 1120 ± 325 >10000
rat FFA reduction (1 h post 1 mg/kg dosing) −77% −14% −80%c
rat TG reduction (1 h post 1 mg/kg dosing) −49% −23% −60%c
dog FFA reduction (1 h post 3 mg/kg dosing) −70% ndb −38%
a

Data represent an average of multiple determinations (n ≥ 3) ± standard deviation.

b

nd = not determined.

c

10 mg/kg dosing.