Table 1 Structural information and in vitro data of IRPA dimers*.

From: Functionally selective signaling and broad metabolic benefits by novel insulin receptor partial agonists

Cmpd

Alternative name

In vitro assays (hIR)

Linker site

Linker

Capping group

IR Bind EC50 (nM)

pAkt EC50 (nM)

pAkt Max Act (%)

RHI

 

—

—

—

0.4

0.07

100

IRPA-1

MK-5160

B29-B29’

C8

NH2(CO)-

6.98

0.12

29

IRPA-2

 

B29-B29’

C8

None

1.34

0.12

43

IRPA-3

 

B29-B29’

C8

CH3(CO)-

2.02

0.13

26

IRPA-4

 

B3-B3’

Trz

None

0.22

0.006

51

IRPA-5

 

B29-B29’

Trz

None

1.09

0.11

37

IRPA-6

 

B1-B29’

Trz

None

0.41

0.04

92

IRPA-7

MK-1092

B29-B29’

cHex

None

2.60

0.14

43

IRPA-8

 

B29-B29’

Peg5

(CH3)2

1.28

0.03

27

IRPA-9

 

B1-B1’

Trz

None

0.53

0.01

96

  1. * Refer to Fig. S1A for the structures of linkers and capping groups. B3 N → K and B29 K → R mutated insulin was used for IRPA-4 (B3–B3′ dimer).
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