Table 2 Human plasma protein binding and rodent S9 microsomal stability for compounds 4 and 5

From: Potent Rifampicin derivatives can clear MRSA infections at single low doses when concomitantly dosed with Vancomycin

Plasma Protein Binding

Compound Number

% Protein Free

% Protein Bound

% Matrix Stability (6 h)

% Recovery (vs. T0 stability)

4

11.8 ± 2

88.2 ± 2

96.5

97.2

5

4.5 ± 0.5

95.5 ± 0.5

89.9

92.4

Rifabutin

10.4 ± 0.5

89.6 ± 0.5

104.9

98.2

Rifampicin

20.9 ± 0.6

79.1 ± 0.6

74.3

81.9

S9 Microsome Stability

Compound Number

Species

T1/2 (min)

% Remaining at T120

CLint (mL/min/kg)

CLint (L/hr/kg)

4

CD-1 Mouse

>120

103.1

<45.5

<2.73

5

CD-1 Mouse

>120

106.4

<45.5

<2.73

Rifabutin

CD-1 Mouse

25

4.6

219

13.1

Rifampicin

CD-1 Mouse

>120

125.1

<45.5

<2.73

4

SD Rat

>120

112.4

<23.4

<1.4

5

SD Rat

>120

102.9

<23.4

<1.4

Rifabutin

SD Rat

1195

89

2.35

0.141

Rifampicin

SD Rat

>120

129.4

<23.4

<1.4

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