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Teneligliptin,DPP-4抑制剂

强效，持久\ xa0DPP-4抑制剂
规格或纯度: 98%
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T127809-500mg 500mg 现货 Stock Image
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dipeptidyl peptidase 4 Inhibitor dipeptidyl peptidase 8 Inhibitor dipeptidyl peptidase 9 Inhibitor
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基本描述

规格或纯度 98%
英文名称 Teneligliptin
别名 特力利汀
生化机理 Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Dipeptidyl peptidase-4 (DPP-4) inhibitors have been demonstrated to improve glycemic control, in particular postprandial hyperglycemic control, in patients with type 2 diabetes. Studies indicate that teneligliptin is a potent, competitive, and long-lasting DPP-4 inhibitor that improves postprandial hyperglycemia and dyslipidemia by both single and repeated administrations.Potent, long-lasting\xa0DPP-4\xa0(dipeptidylpeptidase-4) inhibitor. Competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro ( IC 50 = ~\xa01 nM).
储存温度 -20°C储存
运输条件 超低温冰袋运输
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

名称和标识符

IUPAC Name [(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone
INCHI InChI=1S/C22H30N6OS/c1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27/h2-6,13,19-20,23H,7-12,14-16H2,1H3/t19-,20-/m0/s1
InChi Key WGRQANOPCQRCME-PMACEKPBSA-N
Canonical SMILES CC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5
分子式

C22H30N6OS
PubChem CID 11949652
分子量 426.58

化学和物理性质

溶解性 DMSO

靶标

Target ID 1612
名称 dipeptidyl peptidase 4
缩写名 SHP2
家族 S9: Prolyl oligopeptidase
别名 levocabastine-sensitive neurotensin receptor
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 766 2q24.2 DPP4 dipeptidyl peptidase 4
Mouse 1 760 2 35.85 cM Dpp4 dipeptidylpeptidase 4
Rat 1 767 3q21 Dpp4 dipeptidylpeptidase 4
Ensembl Gene ENSG00000197635 (Hs) , ENSMUSG00000035000 (Mm) , ENSRNOG00000030763 (Rn)
Entrez Gene 13482 (Mm) , 25253 (Rn) , 1803 (Hs)
OMIM 102720 (Hs)
Protein GI 6978773 (Rn) , 227116292 (Mm) , 18765694 (Hs)
UniProtKB P27487 (Hs) , P28843 (Mm) , P14740 (Rn)
RefSeq Protein NP_001926 (Hs) , NP_001153015 (Mm) , NP_034204 (Mm) , NP_036921 (Rn)
RefSeq Nucleotide NM_001935 (Hs) , NM_001159543 (Mm) , NM_010074 (Mm) , NM_012789 (Rn)
MEROPS S09.003 (Hs)
DrugBank Target P27487 (Hs)
CATH/Gene3D 3.40.50.1820 (N/A)
ChEMBL Target CHEMBL4653 (Rn) , CHEMBL284 (Hs) , CHEMBL3883 (Mm)
Target ID 2356
名称 dipeptidyl peptidase 8
缩写名 SHP2
家族 S9: Prolyl oligopeptidase
别名 levocabastine-sensitive neurotensin receptor
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 898 15q22.31 DPP8 dipeptidyl peptidase 8
Mouse 2 892 9 C Dpp8 dipeptidylpeptidase 8
Rat 2 147 8q24 Dpp8 dipeptidylpeptidase 8
OMIM 606819 (Hs)
Entrez Gene 54878 (Hs) , 74388 (Mm)
UniProtKB Q6V1X1 (Hs) , Q80YA7 (Mm)
RefSeq Protein NP_060213 (Hs) , NP_569118 (Hs) , NP_932064 (Hs) , NP_932065 (Hs) , NP_083182 (Mm)
RefSeq Nucleotide NM_017743 (Hs) , NM_130434 (Hs) , NM_197960 (Hs) , NM_197961 (Hs) , NM_028906 (Mm)
Ensembl Gene ENSG00000074603 (Hs) , ENSMUSG00000032393 (Mm) , ENSRNOG00000019105 (Rn)
MEROPS S09.018 (Hs)
Protein GI 18450278 (Hs) , 18450280 (Hs) , 37577089 (Hs) , 37577091 (Hs) , 31542571 (Mm)
CATH/Gene3D 3.40.50.1820 (N/A)
ChEMBL Target CHEMBL4657 (Hs)
Target ID 2357
名称 dipeptidyl peptidase 9
缩写名 SHP2
家族 S9: Prolyl oligopeptidase
别名 levocabastine-sensitive neurotensin receptor
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 863 19p13.3 DPP9 dipeptidyl peptidase 9
Mouse 2 862 17 D Dpp9 dipeptidylpeptidase 9
Rat 2 147 9q11 Dpp9 dipeptidyl peptidase 9
OMIM 608258 (Hs)
Entrez Gene 91039 (Hs) , 224897 (Mm) , 301130 (Rn)
UniProtKB Q86TI2 (Hs) , Q8BVG4 (Mm)
RefSeq Protein NP_631898 (Hs) , NP_766212 (Mm)
RefSeq Nucleotide NM_139159 (Hs) , NM_172624 (Mm)
Ensembl Gene ENSG00000142002 (Hs) , ENSMUSG00000001229 (Mm) , ENSRNOG00000050748 (Rn)
MEROPS S09.019 (Hs)
Orphanet 353250 (Hs)
Protein GI 194394146 (Hs) , 255003757 (Mm)
CATH/Gene3D 3.40.50.1820 (N/A)
ChEMBL Target CHEMBL3259484 (Mm) , CHEMBL4793 (Hs)

关联配体

Ligand ID 9906
名称 teneligliptin
别名 MP-513
类别 Synthetic organic
学名 [(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Teneligliptin is a long-acting, orally bioavailable dipeptidyl peptidase 4 (DPP-4) inhibitor . It was developed for clinical potential in type 2 diabetes management, to improve glycemic control. In addition to their anti-diabetic activity, DPP4 inhibitors may have renal and cardiovascular protective effects.

参考文献

1. Yoshida T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N, Sekiguchi S et al..  (2012)  Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes..  Bioorg Med Chem,  20  (19):  (5705-19).  [PMID:22959556]
2. Salim HM, Fukuda D, Higashikuni Y, Tanaka K, Hirata Y, Yagi S, Soeki T, Shimabukuro M, Sata M.  (2017)  Teneligliptin, a dipeptidyl peptidase-4 inhibitor, attenuated pro-inflammatory phenotype of perivascular adipose tissue and inhibited atherogenesis in normoglycemic apolipoprotein-E-deficient mice..  Vascul Pharmacol,  96-98  (13):  (19-25).  [PMID:28347868]
3. Haneda M, Kadowaki T, Ito H, Sasaki K, Hiraide S, Ishii M, Matsukawa M, Ueno M.  (2018)  Safety and Efficacy of Teneligliptin in Patients with Type 2 Diabetes Mellitus and Impaired Renal Function: Interim Report from Post-marketing Surveillance..  Diabetes Ther,  9  (3):  (1083-1097).  [PMID:29637459]
4. Pan X et al..  (2019)  Essential Role Of High Glucose-Induced Overexpression Of PKC? And PKCd In GLP-1 Resistance In Rodent Cardiomyocytes..  Diabetes Metab Syndr Obes,  12  ():  (2289-2302).  [PMID:31807042]

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