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Delequamine 119905-05-4

Delequamine 119905-05-4

CAS No.: 119905-05-4

Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for ra
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Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for rat cortical α2-adrenergic receptors. Delequamine is more than 1000-fold selective for 5-HT1A receptors and α1-adrenergic receptors. Delequamine can be used in the study of erectile dysfunction.

Physicochemical Properties


Molecular Formula C18H26N2O3S
Molecular Weight 350.48
CAS # 119905-05-4
Related CAS # rel-Delequamine;Delequamine hydrochloride
SMILES

COC1C=CC2[C@@H]3C[C@@H]4N(S(=O)(C)=O)CCC[C@@H]4CN3CCC=2C=1

Synonyms

RS-15385-197
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets α2-adrenergic receptor 9.5 (pKi) α1-adrenergic receptor 5.3 (pKi)
ln Vivo Delequamine (0.4-6.4 mg/kg; oral, single dose) increases sexual behavior scores in a dose-dependent manner in a model in which untrained male rats are exposed to estrogen-progestin treated, sexually receptive female rats. Delequamine (0.4 mg/kg; oral; single dose) combined with 8-OH-DPAT (0.1 mg/kg; subcutaneous injection) increases the percentage of mounting, penetration, and ejaculation, shortens the latency to ejaculation, and reduces the number of penetrations in rats [1].
References

[1]. Modulation of sexual behaviour in the rat by a potent and selective alpha 2-adrenoceptor antagonist, delequamine (RS-15385-197). Br J Pharmacol. 1996;118(1):63-72.


Solubility Data


Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8532 mL 14.2661 mL 28.5323 mL
5 mM 0.5706 mL 2.8532 mL 5.7065 mL
10 mM 0.2853 mL 1.4266 mL 2.8532 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.