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Deriglidole

Catalog No. T10998   CAS 122830-14-2
Synonyms: SL 86-0715

Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.

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Deriglidole Chemical Structure
Deriglidole, CAS 122830-14-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 460.00
5 mg In stock $ 1,060.00
10 mg In stock $ 1,420.00
25 mg In stock $ 2,100.00
50 mg In stock $ 2,580.00
100 mg In stock $ 3,400.00
1 mL * 10 mM (in DMSO) In stock $ 792.00
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Purity: 99.45%
Purity: 98.72%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Deriglidole (SL 86-0715) is a peripheral adrenergic receptor antagonist that is a selective inhibitor of alpha2 receptors. Deriglidole inhibits colistin and Idazoxan but does not show activity against prazosin and rat cortical and human platelet α2-adrenergic receptors.
In vitro Deriglidole is a specific inhibitor of α2-receptors. Deriglidole inhibits the binding of [3H] clonidine and [3H] imidazole x, while showing no inhibitory effect on the binding of [3H] prazosin to rat cortex and human platelet α2-adrenergic receptors. Furthermore, it demonstrates greater effectiveness than idazolide in selectively targeting peripheral receptors.[1]
In vivo In mouse pancreatic beta-cells that both deriglidole and SL86.0714 inhibit ATP-sensitive K+ channel with similar potency whereas alpha2-adrenoceptors are blocked only by deriglidole. In diabetic rats, SL84.0418 and deriglidole (10 mg/kg i.p.) fully normalized glucose tolerance whereas SL86.0714 and tolbutamide only slightly improved it. Five min after deriglidole administration in mice a marked and short lasting rise in insulin levels was observed, followed by a progressive reduction of glycemia.[2]
Synonyms SL 86-0715
Molecular Weight 255.36
Formula C16H21N3
CAS No. 122830-14-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32.5 mg/mL (127.27 mM)

TargetMolReferences and Literature

1. Natali A, et al. Effects of acute alpha 2-blockade on insulin action and secretion in humans. Am J Physiol. 1998;274(1):57-64. 2. Guillot E, et al. Mechanisms of the hypoglycemic effects of the alpha2-adrenoceptor antagonists SL84.0418 and deriglidole. Life Sci. 1998;62(9):839-852. 3. Jonas JC, et al. The imidazoline SL 84.0418 shows stereoselectivity in blocking alpha 2-adrenoceptors but not ATP-sensitive K+ channels in pancreatic B-cells. Eur J Pharmacol. 1994;264(1):81-84.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Inhibitor Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

Deriglidole 122830-14-2 GPCR/G Protein Neuroscience Adrenergic Receptor SL 86-0715 inhibitor inhibit

 

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