Dorzagliatin

Product Name: Dorzagliatin
CAS No.: 1191995-00-2
Chemical Name: Dorzagliatin
Synonyms: RO-5305552;Dorzagliatin;Dorzagliatin, 10 mM in DMSO;Dorzagliatin (Synonyms: HMS5552);DORZAGLIATIN;1191995-00-2;DORZAGLIATIN; SINOGLIATIN ;HMS5552; RO5305552;(S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihyd;(S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-MethylpentanaMide;diabetes,inhibit,β-cell,Hexokinase IV,Inhibitor,glycaemic,type 2,Hexokinase D,Glucokinase,Dorzagliatin,pancreatic,HMS-5552,HMS 5552;(S)-2-[4-(2-chloro-phenoxy)-2-oxo-2,5-dihydro-pyrrol-1-yl]-4-methyl-pentanoic acid [1-((R)-2,3-dihydroxy-propyl)-1H-pyrazol-3-yl]-amide;1H-Pyrrole-1-acetamide, 4-(2-chlorophenoxy)-N-[1-[(2R)-2,3-dihydroxypropyl]-1H-pyrazol-3-yl]-2,5-dihydro-α-(2-methylpropyl)-2-oxo-, (αS)-
CBNumber: CB52658686
Molecular Formula: C22H27ClN4O5
Formula Weight: 462.93
MOL File: 1191995-00-2.mol

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Dorzagliatin Property

Boiling point:: 761.7±60.0 °C(Predicted)
Density: 1.38±0.1 g/cm3(Predicted)
solubility: DMSO:108.5(Max Conc. mg/mL);234.38(Max Conc. mM)
Ethanol:92.0(Max Conc. mg/mL);198.73(Max Conc. mM)
pka: 12.84±0.70(Predicted)
form: Solid
color: White to off-white

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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.

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N-Bromosuccinimide Price

Biosynth Carbosynth

Product number: BD167920
Product name: Dorzagliatin
Packaging: 10mg
Price: $115
Updated: 2021/12/16

ChemScene

Product number: CS-0030544
Product name: Dorzagliatin
Purity: 99.68%
Packaging: 10mg
Price: $180
Updated: 2021/12/16

ChemScene

Product number: CS-0030544
Product name: Dorzagliatin
Purity: 99.68%
Packaging: 25mg
Price: $320
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BD167920
Product name: Dorzagliatin
Packaging: 50mg
Price: $399
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: CCH0033785
Product name: (S)-2-(4-(2-CHLOROPHENOXY)-2-OXO-2,5-DIHYDRO-1H-PYRROL-1-YL)N-(1-((R)-2,3-DIHYDROXYPROPYL)-1H-PYRAZOL-3-YL)-4-METHYLPENTANAMIDE
Purity: 95.00%
Packaging: 5MG
Price: $499.37
Updated: 2021/12/16

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Dorzagliatin Chemical Properties,Usage,Production

Description

Dorzagliatin (trade name HuaTangNing) is a first-in-class small molecule oral glucokinase activator (GKA) developed by Hua Medicine for the treatment of diabetic nephropathy (DKD), type 1 diabetes mellitus (T1DM) and type 2 diabetes mellitus (T2DM). Dorzagliatin was first approved in China in September 2022 as a monotherapy or in combination with metformin, an antidiabetic drug, for adults with type 2 diabetes.

Uses

Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes[1].

Mechanism of action

The mechanism of action of dolagliflozin is through the activation of glucokinase, an enzyme that plays a key role in blood sugar regulation. By increasing the activity of glucokinase, dolagliflozin helps improve blood sugar control, especially in situations where blood sugar rises after a meal.

Synthesis

First, ethyl 2-butynoate was subjected to base-mediated olefination of 2-chlorophenol (18.5) to afford the ester 18.6 (Figure 5.2.2). Subsequent bromination with NBS and AIBN afforded the allylic bromide 18.7. Next, L-leucine methyl ester hydrochloride (18.8) was added to the base to afford the free amine, which underwent allylation with the bromide 18.7. The acid 18.9 was generated via cyclization-condensation and hydrolysis with NaOH. EDCI and HOBt promoted the formation of the final amide bond to afford the amide 18.10, and the 1,2-diol was subjected to acid-mediated acetone deprotection to afford dogliflozin (18) on a 100 kg scale.

in vivo

Dorzagliatin (low-dose 10?mg/kg, and high-dose 30?mg/kg; administered intragastrically; daily 8:00 AM for one month) exerts a glucose-lowering effect on the glucose levels in diabetic rats^[2.

Animal Model:	Male Sprague-Dawley (SD) rats (aged approximately 6–8 weeks and weighing 200-230?g)^[2
Dosage:	Low-dose (10?mg/kg), and high-dose (30?mg/kg)
Administration:	Administered intragastrically (i.g.); daily (8:00 AM) for one month
Result:	Exerted a glucose-lowering effect on the glucose levels.

References

[1] Zhu XX, et al. Dorzagliatin (HMS5552), a novel dual-acting glucokinase activator, improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes: A 28-day treatment study using biomarker-guided patient selection. Diabetes Obes DOI:10.1111/dom.13338
[2] Wang P, et al. Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J Diabetes Res. 2017;2017:5812607. DOI:10.1155/2017/5812607

Dorzagliatin Preparation Products And Raw materials

Raw materials

Preparation Products

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Dorzagliatin Suppliers

China 61 United States 3 Global 64

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4765
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185;
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3505
Advantage: 58

Shanghai Balmxy Pharmaceutical Co., Ltd

Tel: 021-24206007 13764915196
Fax: 86-021-23027023
Email: sales@balmxy.com
Country: China
ProdList: 6897
Advantage: 55

Shanghai Macklin Biochemical Co.,Ltd.

Tel: 15221275939
Fax: 021-50706099
Email: shenlinxing@macklin.cn
Country: China
ProdList: 15872
Advantage: 55

ShangHai Angti Biotechnology Co., Ltd.

Tel: 13764913901
Fax: -
Email: info@angtibio.com
Country: China
ProdList: 4977
Advantage: 55

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

Jinan elephant international trading co., LTD

Tel
Fax: -
Email: 13006575422@163.com
Country: China
ProdList: 6355
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Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 9531
Advantage: 58

Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131957
Advantage: 58

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View Lastest Price from Dorzagliatin manufacturers

Career Henan Chemical Co

Product: (S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-MethylpentanaMide 1191995-00-2
Price: US $7.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 100KG
Release date: 2020-01-13

1191995-00-2, DorzagliatinRelated Search:

(S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihyd

(S)-2-[4-(2-chloro-phenoxy)-2-oxo-2,5-dihydro-pyrrol-1-yl]-4-methyl-pentanoic acid [1-((R)-2,3-dihydroxy-propyl)-1H-pyrazol-3-yl]-amide

(S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-MethylpentanaMide

RO-5305552

DORZAGLIATIN;1191995-00-2;DORZAGLIATIN; SINOGLIATIN ;HMS5552; RO5305552

1H-Pyrrole-1-acetamide, 4-(2-chlorophenoxy)-N-[1-[(2R)-2,3-dihydroxypropyl]-1H-pyrazol-3-yl]-2,5-dihydro-α-(2-methylpropyl)-2-oxo-, (αS)-

diabetes,inhibit,β-cell,Hexokinase IV,Inhibitor,glycaemic,type 2,Hexokinase D,Glucokinase,Dorzagliatin,pancreatic,HMS-5552,HMS 5552

Dorzagliatin (Synonyms: HMS5552)

Dorzagliatin, 10 mM in DMSO

Dorzagliatin

1191995-00-2