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Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $35 | In Stock | |
5 mg | $90 | In Stock | |
10 mg | $146 | In Stock | |
25 mg | $343 | In Stock | |
50 mg | $549 | In Stock | |
100 mg | $828 | In Stock |
Description | Almorexant hydrochloride (ACT 078573 hydrochloride) is an orally active dual orexin receptor antagonist that blocks the intracellular Ca2+ signaling pathway and, to a certain extent, blocks the excitatory effects of methamphetamine. Almorexant hydrochloride Induces apoptosis and can be used to study sleep disorders. |
Targets&IC50 | OX1:1.3 nM(ki), OX2:0.17 nM(ki) |
In vitro | AsPC-1 cells preincubated or not with the SHP2 inhibitor NSC-87877 (50 μM) were challenged for 5 min without or with 1 μM orexin-A or 1 μM Almorexant hydrochloride. In parallel, HPAF-II cells were also challenged for 5 min without or with 1 μM orexin-A. Orexin-A and Almorexant hydrochloride promote tyrosine phosphorylation of SHP2/OX1R complex. [1] |
In vivo | Daily intraperitoneal injection of Almorexant hydrochloride (1.8 μmol/kg) at day 0 in mice xenografted with AsPC-1 cells and up to the mice sacrifices resulted in a significant decrease in tumor volume (> 50%), as compared to untreated mice. Treatment with Almorexant hydrochloride started after AsPC-1 tumors were developed, rapidly and strongly reduced the volume of established tumors. OX1R expression revealed by immunodetection was not affected by Almorexant hydrochloride treatment. [1] |
Alias | Orexin-RA-1 hydrochloride, ACT-078573 hydrochloride, ACT 078573 hydrochloride, A 573 hydrochloride |
Molecular Weight | 549.02 |
Formula | C29H32ClF3N2O3 |
Cas No. | 913358-93-7 |
Smiles | C(CC1=CC=C(C(F)(F)F)C=C1)[C@H]2C=3C(=CC(OC)=C(OC)C3)CCN2[C@@H](C(NC)=O)C4=CC=CC=C4.Cl |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 48 mg/mL (87.4 mM) DMSO: 40 mg/mL (72.86 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO/Ethanol
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