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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
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 the degree 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
If you know of a relevant reference for Org 20599, please let us know.
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Keywords: Org 20599, Org 20599 supplier, Positive, allosteric, modulators, direct, agonists, GABAA, receptors, Receptors, Org20599, PAM, 2738, Tocris Bioscience
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