Table 3.
Profiling data of NPs and SAR‐compounds.
|
|
Log D [d] |
Microsomal stability[d] |
Caco‐2 permeability[d] |
Cytotoxicity[d] |
|||
|---|---|---|---|---|---|---|---|
|
|
pH 7.4 |
CLint [μL/min/mg protein] (t1/2 [min]) |
Papp [10−7 cm s−1] (recovery [%]) |
TC50 [μM] |
|||
|
|
Human |
Mouse |
A2B |
+Elacridar |
THP1 |
HepG2 |
|
|
3 |
4.11 |
[c] |
[c] |
[b] |
[c] |
[c] |
[c] |
|
4 |
4.01 |
72.7 (19.1) |
349 (3.97) |
41.1 (10.1) |
56.2 (14.2) |
5.84 |
4.5 |
|
27 |
4.14 |
95.8 (14.5) |
1500 (0.924) |
117 (42.1) |
87.7 (38.5) |
10.6 |
10.7 |
|
ent‐4 |
3.97 |
26.9 (51.6) |
271 (5.12) |
73.5 (23.4) |
46.7 (28.7) |
8.78 |
5.97 |
|
ent‐27 |
4.16 |
44.3 (31.3) |
764 (1.81) |
40.5 (8.69) |
64.4 (15.3) |
11.5 |
10.4 |
|
35 |
4.7 |
45.5 (30.5) |
1040 (1.33) |
135 (76.0) |
181 (29.6) |
12.9 |
9.39 |
|
36 |
4.73 |
39.7 (34.9) |
259 (5.36) |
[b] (16.1) |
[b] (19.9) |
15.1 |
16.1 |
|
ent‐35 |
4.72 |
40.5 (34.3) |
561 (2.47) |
162 (37.2) |
[b] (46.1) |
12.9 |
14.7 |
|
ent‐36 |
4.74 |
29.9 (46.3) |
721 (1.92) |
8.55 (14.3) |
12.4 (12.0) |
18.2 |
11.3 |
|
37 |
2.82 |
54.6 (25.4) |
[a] |
326 (74.8) |
279 (80.9) |
27.2 |
30 |
|
38 |
2.84 |
76.0 (18.2) |
1070 (1.29) |
620 (127) |
331 (132) |
30 |
9.49 |
|
ent‐37 |
2.82 |
73.5 (18.9) |
370 (3.75) |
360 (81.3) |
300 (74.6) |
25.2 |
30 |
|
2 |
2.86 |
150 (9.26) |
[a] |
407 (86.7) |
393 (83.4) |
30 |
>30 |
[a] Test compound not detectable by 5 minutes. Unable to determine CLint. [b] No data obtained. [c] Not determined. [d] For measurement details and standard deviations of biological data see Supporting Information.