Org 20599

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Cat.No. 2738 - Org 20599 | C25H40ClNO3 | CAS No. 156685-94-8
Description: Positive allosteric modulator of GABAA receptors; direct agonist at higher concentrations
Chemical Name: (2β,3α,5α)-21-Chloro-3-hydroxy-2-(4-morpholinyl)pregnan-20-one
Datasheet
Citations
Reviews
Literature

Biological Activity

Positive allosteric modulator and at higher concentrations direct agonist of GABAA receptors (EC50 = 1.1 μM). Also displays positive modulation of glycine receptors (EC50 = 22.9 μM). Anesthetic steroid; induces hypnosis and loss of righting reflexes in mice.

Technical Data

M. Wt 438.04
Formula C25H40ClNO3
Storage Store at RT
CAS Number 156685-94-8
PubChem ID 9850026
InChI Key NZFNABGZEQPYBX-PMBZPZLSSA-N
Smiles O=[C@](CCl)[C@H]4CC[C@@]3([H])[C@]2([H])CC[C@@]1([H])C[C@H](O)[C@@H](N5CCOCC5)C[C@@](C)1[C@]([H])2CC[C@@]34C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 43.8 100
DMSO 43.8 100

Preparing Stock Solutions

The following data is based on the product molecular weight 438.04. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.28 mL 11.41 mL 22.83 mL
5 mM 0.46 mL 2.28 mL 4.57 mL
10 mM 0.23 mL 1.14 mL 2.28 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References

References are publications that support the biological activity of the product.

Hill-Venning et al (1996) The anaesthetic action and modulaton of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology 35 1209 PMID: 9014136

Visser et al (2002) Neuroactive steroids differ in potency but not in intrinsic efficacy at the GABAA receptor in vivo. J.Pharmacol.Exp.Ther. 303 616 PMID: 12388643

Weir et al (2004) The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors. Br.J.Anaesth. 92 704 PMID: 15033889


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