Category
Insulin
ID
NNC0121-0038
Amount per vial
2000 nmol
Insulin is a peptide hormone acting as a key regulator of glucose homeostasis. Insulin binds to the insulin receptor (InsR), which exists in two alternatively spliced isoforms, InsR-A and InsR-B. The insulin receptor belongs to the same family of receptor tyrosine kinases as the IGF1 receptor (IGF1R) and insulin is therefore also able to bind to the IGF1R albeit with considerably lower affinity as compared to the insulin receptor.
NNC0121-0038 is a very low affinity insulin analogue in which the phenylalanine in position 25 of the B-chain is mutated to aspartic acid causing NNC0121-0038 to bind the insulin receptor with ~2000-fold lower affinity than human insulin.Category
Insulin
ID
NNC0121-0038
Amount per vial
2000 nmol
Property | NNC0121-0038 | Human insulin |
MW (Da) | 5775 | 5808 |
pI | 5.0 | 5.7 |
Sequence substitutions | B25D | - |
Sum formula | C252 H379 N65 O79
S6 | C257 H383 N65 O77 S6 |
Figure 1
2D sketch of NNC0121-0038. Compared to human insulin, the amino acid at position 25 of the B-chain has been changed from phenylalanine to aspartic acid.The single amino acid mutation (phenylalanine to aspartic acid) at position 25 of the B-chain causes a major decrease in insulin receptor as well as IGF1 receptor affinity of NNC0121-0038 which is < 0.05% relative to the affinity of human insulin (see the Drejer K et al. reference listed in the reference section below).
NNC0121-0038 has been tested in vivo by subcutaneous injections in prediabetic NOD mice as described by Karounos DG et al. reference listed in the reference section below.