Anagliptin
- CAS No.
- 739366-20-2
- Chemical Name:
- Anagliptin
- Synonyms
- Suiny;SK-0403;Anagliptin;SUINY;SK-0403;Anagliptin API;Anagliptin (SK-0403);(S)-N-(2-(2-(2-cyanopyrrolidin-1-yl)-2-oxoethylaMino)-2-Methylpropyl)-2-Methylpyrazolo[1,5-a]pyriMidine-6-carboxaMide;(R)-N-(2-(2-(2-cyanopyrrolidin-1-yl)-2-oxoethylamino)-2-methylpropyl)-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide;N-[2-[[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide;N-[2-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide
- CBNumber:
- CB52627327
- Molecular Formula:
- C19H25N7O2
- Molecular Weight:
- 383.45
- MDL Number:
- MFCD19443729
- MOL File:
- 739366-20-2.mol
- MSDS File:
- SDS
| Melting point | 115 - 119°C |
|---|---|
| Density | 1.33±0.1 g/cm3(Predicted) |
| storage temp. | Refrigerator |
| solubility | Chloroform (Slightly), Dichloromethane (Slightly), DMSO (Slightly) |
| form | Solid |
| pka | 12.40±0.46(Predicted) |
| color | White to Off-White |
| FDA UNII | K726J96838 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P280-P305+P351+P338 |
Anagliptin price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | A637210 | Anagliptin | 739366-20-2 | 1mg | $80 | 2021-12-16 | Buy |
| Biosynth Carbosynth | FA31542 | Anagliptin | 739366-20-2 | 2mg | $100 | 2021-12-16 | Buy |
| Biosynth Carbosynth | FA31542 | Anagliptin | 739366-20-2 | 5mg | $200 | 2021-12-16 | Buy |
| ChemScene | CS-4510 | Anagliptin ≥97.0% | 739366-20-2 | 10mg | $240 | 2021-12-16 | Buy |
| Biosynth Carbosynth | FA31542 | Anagliptin | 739366-20-2 | 10mg | $350 | 2021-12-16 | Buy |
Anagliptin Chemical Properties,Uses,Production
Description
Anagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that was approved in Japan in November 2012 for the treatment of patients with Type 2 diabetes mellitus (T2DM). Anagliptin (also known asSK-0403) is a treatment for diabetes based on inhibition of DPP-4, an enzyme that is responsible for degradation of glucagon-like peptide 1 (GLP-1), a 30-amino acid peptide that is secreted in response to food intake. GLP-1 stimulates insulin secretion and inhibits glucagon secretion, which leads to lower levels of plasma glucose. Following the introduction of the first DPP-4 inhibitor, sitagliptin, in 2006, several members of the gliptin class have been approved worldwide. Anagliptin was discovered from an effort to replace a metabolically labile isoindoline group from an earlier DPP-4 inhibitor series with a stable bioisostere. Anagliptin is a potent DPP-4 inhibitor, with an IC50=3.8 nM and >10,000-fold selectivity over inhibition of DPP-8 and DPP-9.
Originator
Sanwa Kagaku Kenkyusho (Japan)
Uses
Anagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction. It also attenuates atherosclerosis in male apolipoprotein E-deficient mice.
Definition
ChEBI: Anagliptin is an amino acid amide.
brand name
Suiny
Clinical Use
Anagliptin, which is marketed as Beskoa or Suiny, is a dipeptidyl peptidase–IV (DPP-4) inhibitor which was approved in September 2012 and launched in November 2012 in Japan for the treatment of Type II diabetes. The drug was co-developed by three Japanese companies; Kowa, Sanwa Kagaku and JW pharmaceutical. Anagliptin, which is more selective against several recombinant human proteases by comparison to sitagliptin and vildagliptin, has more than 10,000-fold selectivity over the structurally homologous DPP-8 and DPP-9 enzymes.
Synthesis
The most likely process-scale synthesis has been published and is depicted in Scheme 3.24 Commercially available (S)-1-(2-chloroacetyl)-pyrrolidine-2-carbonitrile (12) was alkylated with t-butyl (2-amino-2-methyl-1-propyl)carbamate (13), giving rise to (S)-t-butyl (2-((2-(2-cyanopyrrolidin-1-yl)-2- oxoethyl)amino)-2-methylpropyl)carbamate (14). This Boc-protected system was subsequently treated with strong acid to give the ethylene diamine derivative 15 in 96% yield. Activation of 15 with CDI followed by coupling with commercially available 2-methylpyrazolo[1,5-a] pyrimidine-6-carboxylic acid (16) gave anagliptin (III) in 90% yield.
Anagliptin Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 | info@fdachem.com | China | 18214 | 58 |
| Shanghai Time Chemicals CO., Ltd. | +86-021-57951555 +8617317452075 | jack.li@time-chemicals.com | China | 1807 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32715 | 60 |
| Anqing Chico Pharmaceutical Co., Ltd. | 15380796838 | chloewu@chicopharm.cn | CHINA | 341 | 58 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Nanjing Dolon Biotechnology Co.,Ltd. | 18905173768 | sales@dolonchem.com | CHINA | 2972 | 58 |
| Jinan Shengqi pharmaceutical Co,Ltd | 86+18663751872 | christine@shengqipharm.com | CHINA | 491 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| HubeiwidelychemicaltechnologyCo.,Ltd | 18627774460 | faith@widelychemical.com | CHINA | 742 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | sales@chemdad.com | China | 39916 | 58 |
View Lastest Price from Anagliptin manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-04-16 | Anagliptin
739366-20-2
|
US $5.00-0.10 / KG | 1KG | 99% | g-kg-tons, free sample is available | Henan Fengda Chemical Co., Ltd | |
 |
2023-04-19 | Anagliptin
739366-20-2
|
US $50.00 / kg | 1kg | 99% | 50 tons | Hebei Duling International Trade Co. LTD | |
 |
2023-01-31 | Anagliptin
739366-20-2
|
US $100.00 / kg | 1kg | 99% | 50000KG/month | Hebei Mojin Biotechnology Co., Ltd |
-
- Anagliptin
739366-20-2
- US $5.00-0.10 / KG
- 99%
- Henan Fengda Chemical Co., Ltd
-
- Anagliptin
739366-20-2
- US $50.00 / kg
- 99%
- Hebei Duling International Trade Co. LTD
-
- Anagliptin
739366-20-2
- US $100.00 / kg
- 99%
- Hebei Mojin Biotechnology Co., Ltd