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Diabetes Research
DPP IV Inhibitors

 

Dipeptidyl peptidase IV (DPP IV) inhibitors are expected to be categorized in a new type of antidiabetic drugs.


INDEX

1. DPP IV Inhibitor 1c Hydrochloride
2. NVP-DPP728 Dihydrochloride
3. K579
4. Berberine Chloride
5. Product List

1. DPPIV Inhibitor 1c Hydrochloride
(Wako Catalog No. 044-31291 (5 mg))

An achiral, slow-binding (time-dependent) inhibitor of DPP IV that is selective for DPP IV over other DPP isozymes and proline specific serine proteases. The hydrochloride salt of 1c was further profiled for development as a potential new treatment for type 2 diabetes.
  • Appearance: White ~ slightly yellow, crystals ~ powder or mass
  • Assay (HPLC): 95.0+ %
  • IC50 = 104 nmol/L
  • Solubility: Soluble in water, DMSO and ethanol.
[Reference]
Wright SW, Ammirati MJ, Andrews KM, et al.: "cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization", J. Med. Chem., 49, 3068-76 (2006).


(2S,5R)-1-[1-(Hydroxymethyl)cyclopenthylamino]acetyl-2,5-pyrrolidinedicarbonitrile Hydrochloride
C14H20N4O2 · HCl = 312.80

2. NVP-DPP728 Dihydrochloride
(Wako Catalog No. 142-08851 (5 mg))

A dipeptidyl peptidase IV (DPP IV) inhibitor.  With IC50 = 14 nmol/L, high selectivity 15,000 times or more than the inhibitory activity to DPP II is shown.  DPP IV is an enzyme that degrades glucagon-like peptide 1 (GLP-1), an insulin secretion promoter, and DPP IV inhibitors have been studied as therapeutics for diabetes mellitus.
  • Appearance: White ~ slightly pale brown, Crystals ~ powder
  • Assay (Titration): 95.0+ %
  • IC50 = 14 nmol/L
  • Solubility: Soluble in methanol
[Reference]
Hughes, TE, Mone, MD, Russell, ME, Weldon, SC and Villhauer, EB: "NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano- (S)-pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV", Biochemistry, 38, 11597-11603 (1999).


((2S)-1-(2-([5-Cyano-2-pyridyl]amino)ethylamino)acetyl-2-pyrrolidinecarbonitrile Dihydrochloride
C15H18N6O·2HCl = 371.26

3. K579 (Wako Catalog No. 118-00871 (5 mg))

K579 was a more potent and slower binding inhibitor than the existing dipeptidyl peptidase IV inhibitor such as NVP-DPP728.  DPP IV is an enzyme that degrades glucagon-like peptide 1 (GLP-1), an insulin secretion promoter, and DPP IV inhibitors have been studied as therapeutics for diabetes mellitus.
  • Assay (HPLC): 98.0+ %
  • IC50=3 nmol/L (rat); 5 nmol/L (dog); 8 nmol/L (human); 8 nmol/L (monkey)
  • Solubility: Soluble in methanol
[Reference]
Takasaki, K., Iwase, M., Nakajima, T., Ueno, K., Nomoto, Y., Nakanishi, S. and Higo, K.: "K579, a slow-binding inhibitor of dipeptidyl peptidase IV, is a long-acting hypoglycemic agent", Eur. J. Pharmacol., 486, 335 (2004).


(2S)-1-[4-Methyl-1-(2-pyrimidinyl)-4-piperidylamino]acetyl-2-pyrrolidinecarbonitrile
C17H24N6O = 328.41;
CAS No. [440100-64-1]

4. Berberine Chloride (Wako Catalog No. 027-11781 (100 mg))

Berberine was recently reported to potently inhibit the pro-diabetic target human protein tyrosine phosphatase 1B (h-PTP 1B) discloses a novel dual natural h-PTP 1B/DPP IV inhibitor.
  • Appearance: Yellow, crystalline powder ~ powder
  • Assay (HPLC): 90.0+ %
  • Solubility: Freely soluble in boiling water; soluble in hot ethanol; slightly soluble in methanol
[Reference]
Al-masri IM, Mohammad MK, Tahaa MO. and Tahaa MO: "Inhibition of dipeptidyl peptidase IV (DPP IV) is one of the mechanisms explaining the hypoglycemic effect of berberine",J. Enzyme Inhibi. Med. Chem., 24, 1061 (2009).


Benzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium, 5,6-dihydro-9,10-dimethoxy-, chloride (9CI)
C20H18ClNO4 = 371.82
CAS No. [633-65-8]



5. Product List

DDP IV Inhibitors
Product Name Package Size Wako Catalog No. Storage Condition
DPPIV Inhibitor 1c Hydrochloride 5 mg 044-31291 Keep at 2 ~ 10°C in a dark place
NVP-DPP728 Dihydrochloride 5 mg 142-08851
K579 5 mg 118-00871
Berberine Chloride 100 mg 027-11781

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Listed products are for research use only. Do not administer each to human.

 

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