Structure
(CH2COOH-PEG6-CH2COOH, CAS 83824-29-7)
Lesogaberan napadisylate Biochemical
Lesogaberan napadisylate
Purity
98%
Synonyms
Lesogaberan napadisylate; N/A; Lesogaberan napadisylate biochemical
Purity/Purification
98%
CAS
477956-38-0
Targets&IC50
rat GABAA:1.4+/-0.3 uM (Ki), rat GABAB:5.1+/-1.2 nM (Ki), human GABABreceptor:8.6+/-0.77 nM (EC50)
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
Lesogaberan (AZD3355) potently stimulates recombinant human GABA B receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1]. Oral Lesogaberan (0.08mg/mL; 48 hours) protects human islet beta-cells from apoptosis in islet grafts in mice[2]. Lesogaberan (7 umol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1]. Animal Model: Diabetic NOD/scid mice were implanted with human islets[2]. Dosage: 0.08mg/mL. Administration: Oral feeding; 48 hours. Result: Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin + beta-cells in human islet grafts. Animal Model: Female Sprague Dawley rats[1]. Dosage: 7 umol/kg (Pharmacokinetic Analysis). Administration: Oral. Result: High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years
In solvent: -80 degree C for 2 years
Structure
(CH2COOH-PEG6-CH2COOH, CAS 83824-29-7)
Structure
(CH2COOH-PEG6-CH2COOH, CAS 83824-29-7)
Structure
(CH2COOH-PEG6-CH2COOH, CAS 83824-29-7)
Structure
(CH2COOH-PEG6-CH2COOH, CAS 83824-29-7)
Related Product Information for Lesogaberan napadisylate biochemical
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABA B receptor agonist with an EC 50 of 8.6 nM for human recombinant GABA B receptors. The affinity (K i s) of Lesogaberan napadisylate for rat GABA B and GABA A receptors, as measured by displacement of [ 3 H]GABA binding in brain membranes: 5.1 nM and 1.4 uM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
References
1. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
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Product Notes
The Lesogaberan napadisylate (Catalog #AAA228733) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Lesogaberan napadisylate, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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