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Identification
NameInsulin Regular
Accession NumberDB00030  (BIOD00105, BTD00105, DB01383)
Typebiotech
Groupsapproved, experimental, investigational
Description

Insulin regular is a 51 residue peptide hormone, composed of two amino acid chains covalently linked by disulfide bonds. The structure is identical to native human insulin. Recombinant insulin is synthesized by recombinant DNA techncology. Inserting the human insulin gene into the Escherichia coli bacteria or Saccharomyces cerevisiae produces insulin for human use.

Protein structureDb00030
Protein chemical formulaC257H383N65O77S6
Protein average weight5808 Daltons
Sequences
>A chain
GIVEQCCTSICSLYQLENYCN
>B chain
FVNQHLCGSHLVEALYLVCGERGFFYTPKT
Download FASTA Format
Synonyms
SynonymLanguageCode
Insulin human Not AvailableNot Available
SaltsNot Available
Brand names
NameCompany
Humulin REli Lilly and Company
Novolin RNovo Nordisk
Brand mixtures
Brand NameIngredients
Humulin 20/8020% human insulin injection; 80% human insulin isophane suspension
Humulin 50/50 50% human insulin isophane suspension; 50% human insulin injection
Humulin 70/30 70% human insulin isophane suspension; 30% human insulin injection
Humulin 70/30 Pen 70% human insulin isophane suspension; 30% human insulin injection
Novolin ge 30/7030% human insulin injection; 70% human insulin isophane suspension
Novolin ge 40/6040% human insulin injection; 60% human insulin isophane suspension
Novolin ge 50/5050% human insulin injection; 50% human insulin isophane suspension
CategoriesNot Available
CAS number11061-68-0
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
IndicationIndicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 1 and type 2 diabetes mellitus.
PharmacodynamicsInsulin regular is a short-acting insulin. When subcutaneously administered, the onset of action (as evidenced by a decrease in glucose level) occurs 30 minutes post-dose. Maximal effect occurs between 1.5 and 3.5 hours post-dose. The glucose-lowering effect occurs 8 hours post-dose. Compared to other rapid-acting insulin analogs, insulin regular has a slower onset of action and longer duration of action.
Mechanism of actionThe primary activity of insulin is the regulation of glucose metabolism. Insulin promotes glucose and amino acid uptake into muscle and adipose tissues, and other tissues except brain and liver. It also has an anabolic role in stimulating glycogen, fatty acid, and protein synthesis. Insulin inhibits gluconeogenesis in the liver. Insulin binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bound receptor is able to autophosphorylate and phosphorylate numerous intracellular substrates such as insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and Gab 1. These activated proteins, in turn, lead to the activation of downstream signaling molecules including PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC) which play a critical role in metabolism and catabolism.
AbsorptionInsulin is generally well absorbed.
Volume of distribution

0.15 L/kg

Protein binding5% protein bound
Metabolism

Insulin is predominantly cleared by metabolic degradation via a receptor-mediated process.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityHypoglycemia is one of the most frequent adverse events experienced by insulin users.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption Not Available Not Available
Blood Brain Barrier Not Available Not Available
Caco-2 permeable Not Available Not Available
P-glycoprotein substrate Not Available Not Available
P-glycoprotein inhibitor I Not Available Not Available
P-glycoprotein inhibitor II Not Available Not Available
Renal organic cation transporter Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 1A2 substrate Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 2C19 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 inhibitory promiscuity Not Available Not Available
Ames test Not Available Not Available
Carcinogenicity Not Available Not Available
Biodegradation Not Available Not Available
Rat acute toxicity Not Available Not applicable
hERG inhibition (predictor I) Not Available Not Available
hERG inhibition (predictor II) Not Available Not Available
Pharmacoeconomics
Manufacturers
  • Novo nordisk inc
Packagers
Dosage forms
FormRouteStrength
InjectionSubcutaneous100 units/mL; 500 units/mL
Prices
Unit descriptionCostUnit
NovoLIN R PenFill 100 unit/ml Solution Five 3ml Cartridges Per Box = 15ml162.26USDcartridge
NovoLIN R 100 unit/ml Solution 10ml Vial73.19USDvial
Novolin r 100 unit/ml cartridg33.33USDml
NovoLIN R InnoLet 100 unit/ml Solution 3ml Cartridge24.17USDcartridge
Humulin N Cartridge 100 unit/ml Cartridge2.99USDcartridge
Humulin R Cartridge 100 unit/ml Cartridge2.99USDcartridge
Novolin Ge Toronto Penfill 100 unit/ml Cartridge2.8USDcartridge
Novolin Ge Nph Penfill 100 unit/ml Cartridge2.78USDcartridge
Humulin N 100 unit/ml2.29USDcartridge
Humulin R 100 unit/ml2.29USDcartridge
Novolin Ge Nph 100 unit/ml2.14USDcartridge
Novolin Ge Toronto 100 unit/ml2.14USDcartridge
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
Stateliquid
Experimental Properties
PropertyValueSource
melting point81 °CKhachidze, D.G. et al., J. Biol. Phys. Chem. 1:64-67 (2001)
hydrophobicity0.218Not Available
isoelectric point5.39Not Available
Spectra
SpectraNot Available
References
Synthesis Reference

Humulin is synthesized in a special non-disease-producing laboratory strain of Escherichia coli bacteria that has been genetically altered to produce human insulin.

General Reference
  1. Herrmann BL, Kasser C, Keuthage W, Huptas M, Dette H, Klute A: Comparison of insulin aspart vs. regular human insulin with or without insulin detemir concerning adipozytokines and metabolic effects in patients with type 2 diabetes mellitus. Exp Clin Endocrinol Diabetes. 2013 Apr;121(4):210-3. doi: 10.1055/s-0033-1334905. Epub 2013 Mar 19. Pubmed
External Links
ResourceLink
UniProtQ8HXV2
GenbankAY137503
PharmGKBPA164744571
Drug Product Database795879
RxListhttp://www.rxlist.com/cgi/generic3/novolog.htm
Drugs.comhttp://www.drugs.com/pro/humulin-r.html
WikipediaInsulin
ATC CodesA10AB01A10AE05A10AB04A10AE04A10AD05A10AC03A10AC01A10AB05A10AB03
AHFS Codes
  • 68:20.08
  • 92:02.00*
PDB Entries
FDA labelshow(133 KB)
MSDSshow(47 KB)
Interactions
Drug Interactions
Drug
LiraglutideCoadministration may increase the risk of hypoglycemia. A lower dose of the antidiabetic agent may be needed.
Food InteractionsNot Available

1. Insulin receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Insulin receptor P06213 Details

References:

  1. Desbuquois B, Chauvet G, Kouach M, Authier F: Cell itinerary and metabolic fate of proinsulin in rat liver: in vivo and in vitro studies. Endocrinology. 2003 Dec;144(12):5308-21. Epub 2003 Sep 11. Pubmed
  2. Chen LM, Yang XW, Tang JG: Acidic residues on the N-terminus of proinsulin C-Peptide are important for the folding of insulin precursor. J Biochem (Tokyo). 2002 Jun;131(6):855-9. Pubmed
  3. Bell DS: Insulin therapy in diabetes mellitus: how can the currently available injectable insulins be most prudently and efficaciously utilised? Drugs. 2007;67(13):1813-27. Pubmed
  4. Tanti JF, Jager J: Cellular mechanisms of insulin resistance: role of stress-regulated serine kinases and insulin receptor substrates (IRS) serine phosphorylation. Curr Opin Pharmacol. 2009 Dec;9(6):753-62. Epub 2009 Aug 13. Pubmed
  5. Chiu SL, Cline HT: Insulin receptor signaling in the development of neuronal structure and function. Neural Dev. 2010 Mar 15;5:7. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Insulin-like growth factor 1 receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Insulin-like growth factor 1 receptor P08069 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

3. Retinoblastoma-associated protein

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Retinoblastoma-associated protein P06400 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

4. Cathepsin D

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Cathepsin D P07339 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

5. Insulin-degrading enzyme

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Insulin-degrading enzyme P14735 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

6. Neuroendocrine convertase 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Neuroendocrine convertase 2 P16519 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

7. Carboxypeptidase E

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Carboxypeptidase E P16870 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

8. Neuroendocrine convertase 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Neuroendocrine convertase 1 P29120 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

9. Protein NOV homolog

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Protein NOV homolog P48745 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

10. Low-density lipoprotein receptor-related protein 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Low-density lipoprotein receptor-related protein 2 P98164 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

11. Insulin-like growth factor-binding protein 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Insulin-like growth factor-binding protein 7 Q16270 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

12. Synaptotagmin-like protein 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Synaptotagmin-like protein 4 Q96C24 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed

1. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

Comments
Drug created on June 13, 2005 07:24 / Updated on June 27, 2013 15:33