New diabetes drugs Uses
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Exendin-4

New diabetes drugs Uses
Product Name
Exendin-4
CAS No.
141758-74-9
Chemical Name
Exendin-4
Synonyms
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2;H-HIS-GLY-GLU-GLY-THR-PHE-THR-SER-ASP-LEU-SER-LYS-GLN-MET-GLU-GLU-GLU-ALA-VAL-ARG-LEU-PHE-ILE-GLU-TRP-LEU-LYS-ASN-GLY-GLY-PRO-SER-SER-GLY-ALA-PRO-PRO-PRO-SER-NH2;XENDIN-4;EXENDIN-4;Exendin-4 >=97%;Exendin-4 Exenatide;Exenatide free base;Exenatide (2.73 mg);Exendin-4 USP/EP/BP;Exenatide (Exendin-4)
CBNumber
CB7738335
Molecular Formula
C184H282N50O60S
Formula Weight
4186.57188
MOL File
141758-74-9.mol
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Exendin-4 Property

RTECS 
VT9545000
storage temp. 
−20°C
solubility 
≥145 mg/mL in DMSO; insoluble in EtOH; ≥52 mg/mL in H2O with gentle warming
form 
White to off-white solid.
Water Solubility 
Soluble in water (1 mg/ml)
InChIKey
HTQBXNHDCUEHJF-AAPNSGCPNA-N
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Safety

WGK Germany 
3
HS Code 
2933290000
Hazardous Substances Data
141758-74-9(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H351Suspected of causing cancer

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
E7144
Product name
Exendin 4
Purity
≥97%
Packaging
0.1mg
Price
$302
Updated
2024/03/01
Sigma-Aldrich
Product number
E7144
Product name
Exendin 4
Purity
≥97%
Packaging
500μg
Price
$894
Updated
2024/03/01
Alfa Aesar
Product number
J66726
Product name
Exendin 4
Packaging
1mg
Price
$313
Updated
2021/12/16
Alfa Aesar
Product number
J66726
Product name
Exendin 4
Packaging
0.5mg
Price
$190
Updated
2021/12/16
Tocris
Product number
1933
Product name
Exendin 4
Packaging
1
Price
$393
Updated
2021/12/16
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Exendin-4 Chemical Properties,Usage,Production

New diabetes drugs

Diabetes is a metabolic disorder characterized by chronic hyperglycemia caused by a variety of causes , high blood sugar is caused by insulin secretion or its effect defect. Diabetes can be divided into type 1 diabetes, type 2 diabetes, other specific types of diabetes, and gestational diabetes, among which type 2 diabetes account for more than 90%.
Exendin-4 is a new diabetes drug successfully developed by American Eli Lilly Company it belongs to incretin analogues, it is the first member of the incretin analogues family , it is the synthetic peptide compound, which can simulate physiological behavior of the natural state secretion of GLP-1 in vivo ,it is similar to human pancreatic glucagon-like peptide effect-1 (GLP-1),it can promote glucose-dependent insulin secretion, it has inhibition effect of inappropriate glucose-dependent glucagon secretion, slowing gastric emptying, it improves the sensitivity of peripheral tissues to insulin, and it makes blood sugar adequately controlled. Clinically it is used for the treatment of type Ⅱ diabetes patients whose blood sugar is unbale to be controlled by metformin, sulfonylurea, or combination of metformin and sulfonylurea.
From April 28, 2005 to October 29, 2008, the US Food and Drug Administration (abbreviation: FDA) Adverse Event Reporting System had received reports of 78 cases of patients with renal exenatide change. In the meantime, the United States had made a total of more than 6.6 million Exendin-4 prescription, therefore, FDA thought the received 78 cases was in a small proportion of the proportion of all patients reporting use of the drug. Currently FDA has completed an assessment of these reported cases, including 62 cases of acute renal failure cases and 16 cases of renal insufficiency cases. Acute renal failure or renal dysfunction occurs three days to two years after treatment. The age span is 23 years to 83 years, mean age is 60 years.
The above information is edited by the chemicalbook of Tian Ye.

Uses

Exendin-4 can activate the GLP-1 receptor, the receptor can increase cAMP levels of pancreatic acinar cells in intracellular , but it has no effect on VIP receptor.

Description

Exendin-4 is a 39 amino acid polypeptide and incretin mimetic involved in the glucose-dependent enhancement of insulin secretion. It was first isolated from Gila monster saliva. It also promotes the reduction of hyperglycemia, glucose-dependent suppression of inappropriately high glucagon secretion, slowing of gastric emptying, and reduction of food intake, often with body weight reduction or blunting of weight gain. The synthetic form, Exenatide, is a glucagon-like peptide-1 (GLP-1) agonist approved for the treatment of diabetes mellitus type II, has a long half-life.

Description

Exenatide is the first drug in a new class of anti-diabetics known as the incretin mimetics, and it is indicated as adjunctive therapy to improve glycemic control in patients with type 2 diabetes who are taking metformin, a sulfonylurea, or both, but have not achieved adequate glycemic control. Exenatide is a functional analog of the human incretin Glucagon-Like Peptide-1 (GLP-1). GLP-1 is naturally released from cells in the GI tract in response to food intake and acts on its receptor on b-cells to potentiate glucose-stimulated insulin secretion. Exenatide is a long-acting agonist at the GLP-1 receptor. It is a synthetic version of a 39-amino acid peptide found in the salivary secretions of the Gila monster lizard.also moderates peak serum glucagon levels during hyperglycemic periods following meals, but does not interfere with glucagon release in response to hypoglycemia. The dosing regimen for exenatide is 5 or 10 mg twice daily, administered as a subcutaneous injection within an hour before morning and evening meals. Following subcutaneous administration, peak plasma concentrations of exenatide are reached in 2.1 h, and the plasma pharmacokinetic profile is dose proportional. The most common adverse events reported with exenatide include nausea, vomiting, diarrhea, feeling jittery, dizziness, headache, and dyspepsia.

Originator

Amylin (US)

Uses

Exendin-4 has been used as incretin mimetics for the treatment in HepG2 cells to exclude the influence of auxiliary material. It has also been used as an r (GLP-1R) agonist to exclude interference from auxiliary material.

Uses

Antidiabetic.

Definition

ChEBI: A bioactive polypeptide of 39 amino acid residues isolated from the saliva of the Gila monster (Heloderma suspectum). High-affinity glucagon-like peptide 1 (GLP-1) receptor agonist (Kd = 136 pM); potently indu es cAMP formation without stimulating amylase release in pancreatic acini; potentiates glucose-induced insulin secretion in isolated rat islets; protects against glutamate-induced neurotoxicity. A synthetic version is called exenatide.

brand name

Byetta

General Description

Exendin-4 is an incretin mimetic peptide, which is composed of 39 amino acids. It is an analog of glucagon-like peptide 1 (GLP-1), and an insulinotropic agent, with a long half-life. Exendin-4 was historically isolated from the venom of Gila monster lizard called Heloderma suspectum.

Biochem/physiol Actions

Activates GLP-1 (glucagon-like peptide-1) receptors to increase intracellular cAMP in pancreatic acinar cells; has no effect on VIP receptors.

in vitro

exendin-4 showed a pronounced effect on intracellular camp generation. treatment of glp-1 in combination with exendin-4 showed additive action on the generation of camp. in isolated rat islets and in mouse insulinoma beta tc-1 cells, exendin-4 stimulated the glucose-induced insulin secretion in a dose dependent manner [2]. in basal forebrain cholinergic neurons, exendin-4 greatly reduced ibotenic acid-induced depletion of choline acetyltransferase immunoreactivity [3].

in vivo

in ob/ob mice, administration of exendin-4 (10 μg/kg or 20 μg/kg) improved insulin sensitivity and significantly reduced serum glucose and hepatic steatosis. exendin-4 appeared to effectively reverse hepatic steatosis in ob/ob mice by improving insulin sensitivity [1]. in athymic mice, 63% of exendin-4-treated mice achieved graft function compared with 21% of untreated mice (p = 0.033) in the short-term study. 88% of treated mice had functioning grafts compared with 22% of controls (p = 0.015) in the long-term study. exendin-4-treated mice gained significantly more weight than the untreated counterparts [4].

storage

-20°C (desiccate)

References

[1]ding x, saxena n k, lin s, et al.  exendin‐4, a glucagon‐like protein‐1 (glp‐1) receptor agonist, reverses hepatic steatosis in ob/ob mice[j]. hepatology, 2006, 43(1): 173-181.
[2]gke r, fehmann h c, linn t, et al.  exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells[j]. journal of biological chemistry, 1993, 268(26): 19650-19655.
[3]perry t a, haughey n j, mattson m p, et al.  protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4[j]. journal of pharmacology and experimental therapeutics, 2002, 302(3): 881-888.sharma a, srenby a, wernerson a, et al.  exendin-4 treatment improves metabolic control after rat islet transplantation to athymic mice with streptozotocin-induced diabetes[j]. diabetologia, 2006, 49(6): 1247-1253.

Exendin-4 Preparation Products And Raw materials

Raw materials

Preparation Products

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Exendin-4 Suppliers

Cellmano Biotech Limited
Tel
0551-65326643 18156095617
Fax
0551-65326641
Email
info@cellmano.com
Country
China
ProdList
1011
Advantage
55
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3750
Advantage
55
Nanjing TGpeptide Biotechnology Co.,Ltd.
Tel
18115476705
Email
sales@tgpeptide.com
Country
China
ProdList
3189
Advantage
58
Shanghai HongTide Biotechnology Co.,Ltd.
Tel
19961912513
Email
sales@hongtide.com
Country
China
ProdList
4524
Advantage
58
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15848
Advantage
69
Alabiochem Tech.Co., Ltd.
Tel
0512-58900862 400-0707518
Fax
0086-512-56765862
Email
sales@alabiochem.com
Country
China
ProdList
995
Advantage
59
GL Biochem (Shanghai) Ltd
Tel
21-61263452 13641803416
Fax
86-21-61263399
Email
ymbetter@glbiochem.com
Country
China
ProdList
9981
Advantage
64
Ascent Scientific
Tel
4401179829988
Fax
4402030 700 369
Email
customerservice@ascentscientific.co.uk
Country
United Kingdom
ProdList
279
Advantage
60
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2127
Advantage
70
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696;
Email
info@hanhongsci.com
Country
China
ProdList
42982
Advantage
64
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View Lastest Price from Exendin-4 manufacturers

Shanghai Affida new material science and technology center
Product
Exendin-4 141758-74-9
Price
US $0.00-0.00/Box
Min. Order
1Box
Purity
99
Supply Ability
50000KG/month
Release date
2024-04-11
Zibo Hangyu Biotechnology Development Co., Ltd
Product
Exendin-4 141758-74-9
Price
US $75.00-750.00/kg
Min. Order
10kg
Purity
0.99
Supply Ability
20tons
Release date
2023-11-01
WUHAN FORTUNA CHEMICAL CO., LTD
Product
Exendin-4 141758-74-9
Price
US $1.00/g
Min. Order
1g
Purity
97.0%-103.0%
Supply Ability
1kg/month
Release date
2021-06-16

141758-74-9, Exendin-4Related Search:


  • H-HIS-GLY-GLU-GLY-THR-PHE-THR-SER-ASP-LEU-SER-LYS-GLN-MET-GLU-GLU-GLU-ALA-VAL-ARG-LEU-PHE-ILE-GLU-TRP-LEU-LYS-ASN-GLY-GLY-PRO-SER-SER-GLY-ALA-PRO-PRO-PRO-SER-NH2
  • HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2
  • Exenatide (Exendin-4)
  • Exenatide free base
  • XENDIN-4
  • EXENDIN-4
  • M.W. 4186.61 C184H282N50O60S
  • HIS-GLY-GLU-GLY-THR-PHE-THR-SER-ASP-LEU-SER-LYS-GLN-MET-GLU-GLU-GLU-ALA-VAL-ARG-LEU-PHE-ILE-GLU-TRP-LEU-LYS-ASN-GLY-GLY-PRO-SER-SER-GLY-ALA-PRO-PRO-PRO-SER-NH2
  • HIS-GLY-GLU-GLY-THR-PHE-THR-SER-ASP-LEU-SER-LYS-GLN-MET-GLU-GLU-GLU-ALA-VAL-ARG-LEU-PHE-ILE-GLU-TRP-LEU-LYS-ASN-GLY-GLY-PRO-SER-SER-GLY-ALA-PRO-PRO-PRO-SER-NH2: HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2
  • Exenatide, AC 2993, Exendin A, ExendinA
  • Exendin-4 Exenatide
  • Exenatide (2.73 mg)
  • Exendin-4 >=97%
  • Exenatide?Acetate impurity
  • Exendin-4 USP/EP/BP
  • Exendin-4 acetate salt
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