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Teneligliptin

CAS No.
760937-92-6
Chemical Name:
Teneligliptin
Synonyms
Teliglietin;teneligliptin;Teneligptin WS;Teneligliptin (MP-513);API (Teneligliptin free base);3-[[(2S,4R)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]carbonyl]thiazolidine;3-[[(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]carbonyl]thiazolidine;Methanone,[(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinyl-;[(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone;((2S,4S)-4-(4-(3-Methyl-1-phenyl1H-pyrazol-5-yl)piperazin-1yl)pyrrolidin-2-yl)(thiazolidin-3yl)methanone hydrobromide hydrate
CBNumber:
CB11518541
Molecular Formula:
C22H30N6OS
Molecular Weight:
426.58
MDL Number:
MFCD13195565
MOL File:
760937-92-6.mol
Last updated:2024-11-19 20:33:22

Teneligliptin Properties

Melting point >100°C (dec.)
Boiling point 663.4±55.0 °C(Predicted)
Density 1.38
storage temp. Refrigerator
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
pka 8.70±0.10(Predicted)
color Off-White
InChIKey WGRQANOPCQRCME-PMACEKPBSA-N
SMILES C([C@@H]1C[C@H](N2CCN(C3N(C4=CC=CC=C4)N=C(C)C=3)CC2)CN1)(N1CCSC1)=O
FDA UNII 28ZHI4CF9C
ATC code A10BH08

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319
Precautionary statements  P264-P280-P302+P352-P305+P351+P338-P332+P313-P337+P313-P362

Teneligliptin price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC T018295 Teneligliptin 760937-92-6 10mg $45 2021-12-16 Buy
ChemScene CS-0882 Teneligliptin 99.57% 760937-92-6 10mg $60 2021-12-16 Buy
ChemScene CS-0882 Teneligliptin 99.57% 760937-92-6 50mg $180 2021-12-16 Buy
ChemScene CS-0882 Teneligliptin 99.57% 760937-92-6 100mg $288 2021-12-16 Buy
American Custom Chemicals Corporation API0014166 TENELIGLIPTIN 95.00% 760937-92-6 5MG $502.54 2021-12-16 Buy
Product number Packaging Price Buy
T018295 10mg $45 Buy
CS-0882 10mg $60 Buy
CS-0882 50mg $180 Buy
CS-0882 100mg $288 Buy
API0014166 5MG $502.54 Buy

Teneligliptin Chemical Properties,Uses,Production

Description

Teneligliptin was approved in September 2012 in Japan for the treatment of patients with Type 2 diabetes mellitus (T2DM). Teneligliptin is a member of the dipeptidyl peptidase 4 (DPP-4) inhibitor class of antidiabetes agents. DPP-4 is an enzyme that degrades 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. Teneligliptin is one of a growing numbers of DPP-4 inhibitors to be approved worldwide. The discovery of teneligliptin was guided by structure-based design, with a key element being binding of the phenyl group in the S2 pocket, which not only increases potency for DPP-4, but also improves selectivity versus DPP-8 and DPP- 9. Teneligliptin is a potent inhibitor of DPP-4 in the enzyme inhibition assay (IC50=0.37 nM).

Originator

Mitsubishi Tanabe Pharma (Japan)

Uses

Teneligliptin, is a dipeptidyl peptidase-4 (DPP-4) inhibitor that is used to treat type 2 diabetes. It is eliminated via excretion, and has a half-life of 24.2 hours in the human body.

Definition

ChEBI: Teneligliptin is an amino acid amide.

brand name

Tenelia

Pharmacokinetics

Reported evidence suggests that with teneligliptin 20 mg therapy, Tmax was 1 hour, and t1/2 was 18.9 hours. Maximum (89.7%) inhibition in plasma DPP-4 activity was noted within 2 hours and maintained >60% at 24 hours. Compared to the placebo, active plasma GLP-1 concentration was higher throughout the day and even 24 hours after administration of 20 mg of teneligliptin. Metabolism of teneligliptin was majorly mediated through CYP3A4, a cytochrome P450 isozyme, and flavin-containing monooxygenases (FMO1 and FMO3). A weak inhibitory activity of teneligliptin on CYP2D6, CYP3A4, and FMO was noted, while there was no inhibitory activity on CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C8/9, CYP2C19, and CYP2E1. There was no induction of expression of CYP1A2 or CYP3A4. Reported evidence suggests that teneligliptin is metabolized and eliminated via renal and hepatic routes. Approximately 34% of teneligliptin is excreted unchanged via the renal route, while 66% is metabolized and eliminated via the hepatic and renal routes[1].

Side effects

The DPP-4 molecule in teneligliptin reduces the risk of hypoglycemia, although it is possible. These are some of teneligliptin’s major and minor side effects:
Hypoglycemia
Headache
Upper respiratory tract infection
Gastrointestinal symptoms
Constipation
Fatigue
Kidney problems
Nasopharyngitis
Skin rashes
Itching
Loss of appetite
Abdominal pain

References

[1] Surendra Kumar Sharma. “Teneligliptin in management of type 2 diabetes mellitus.” Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy 9 (2016): 251–60.

401566-80-1
760937-92-6
Synthesis of Teneligliptin from (2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-(3-thiazolidinylcarbonyl)-1-pyrrolidinecarboxylic acid tert-butyl ester

Teneligliptin Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 187)Suppliers
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ChemExpress
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+8615255079626 eric@witopchemical.com China 23541 58
Xi'an MC Biotech, Co., Ltd.
029-89275612 +8618991951683 mcbio_sales@163.com China 2251 58

Related articles

View Lastest Price from Teneligliptin manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Teneligliptin pictures 2024-11-26 Teneligliptin
760937-92-6
US $0.00-0.00 / kg 1kg 99%, Single impurity<0.1 1 ton Nanjing Fred Technology Co., Ltd
Teneligliptin pictures 2024-11-19 Teneligliptin
760937-92-6
US $0.00-44.00 / mg 10g TargetMol Chemicals Inc.
Teneligliptin pictures 2022-09-16 Teneligliptin
760937-92-6
US $0.00-0.00 / KG 1KG 98% 1ton Henan Aochuang Chemical Co.,Ltd.
  • Teneligliptin pictures
  • Teneligliptin
    760937-92-6
  • US $0.00-0.00 / kg
  • 99%, Single impurity<0.1
  • Nanjing Fred Technology Co., Ltd
  • Teneligliptin pictures
  • Teneligliptin
    760937-92-6
  • US $0.00-44.00 / mg
  • TargetMol Chemicals Inc.
  • Teneligliptin pictures
  • Teneligliptin
    760937-92-6
  • US $0.00-0.00 / KG
  • 98%
  • Henan Aochuang Chemical Co.,Ltd.
teneligliptin 3-[[(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]carbonyl]thiazolidine Methanone,[(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinyl- Teneligptin WS [(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone API (Teneligliptin free base) Teliglietin Teneligliptin (MP-513) 3-[[(2S,4R)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]carbonyl]thiazolidine ((2S,4S)-4-(4-(3-Methyl-1-phenyl1H-pyrazol-5-yl)piperazin-1yl)pyrrolidin-2-yl)(thiazolidin-3yl)methanone hydrobromide hydrate 760937-92-6 C22H30N6OS