Teneligliptin
- Product Name
- 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
- Formula Weight
- 426.58
- MOL File
- 760937-92-6.mol
Teneligliptin Property
- 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
- 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
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- T018295
- Product name
- Teneligliptin
- Packaging
- 10mg
- Price
- $45
- Updated
- 2021/12/16
- Product number
- CS-0882
- Product name
- Teneligliptin
- Purity
- 99.57%
- Packaging
- 10mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- CS-0882
- Product name
- Teneligliptin
- Purity
- 99.57%
- Packaging
- 50mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-0882
- Product name
- Teneligliptin
- Purity
- 99.57%
- Packaging
- 100mg
- Price
- $288
- Updated
- 2021/12/16
- Product number
- API0014166
- Product name
- TENELIGLIPTIN
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $502.54
- Updated
- 2021/12/16
Teneligliptin Chemical Properties,Usage,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.
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Raw materials
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View Lastest Price from Teneligliptin manufacturers
- Product
- Teneligliptin 760937-92-6
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%, Single impurity＜0.1
- Supply Ability
- 1 ton
- Release date
- 2024-01-02
- Product
- Teneligliptin 760937-92-6
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-10
- Product
- Teneligliptin 760937-92-6
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-07-09