Table 1.

Structural information and in vitro data of IRPA dimers*.

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

^* 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).