| Identification | Back Directory | [Name]
LY-2795050 | [CAS]
1346133-08-1 | [Synonyms]
LY2795050
LY-2795050
LY 2795050
LY 2795050; LY-2795050
LY2795050;LY 2795050;LY-2795050;1346133-08-1
3-chloro-4-[4-[ [ (2S)-2-(3-pyridyl)pyrrolidin-1-yl]methyl]phenoxy]benzamide
(S)-3-chloro-4-(4-((2-(pyridin-3-yl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
Benzamide, 3-chloro-4-[4-[[(2S)-2-(3-pyridinyl)-1-pyrrolidinyl]methyl]phenoxy]- | [Molecular Formula]
C23H22ClN3O2 | [MOL File]
1346133-08-1.mol | [Molecular Weight]
407.89 |
| Chemical Properties | Back Directory | [Boiling point ]
532.4±50.0 °C(Predicted) | [density ]
1.287±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (122.58 mM; Need ultrasonic) | [form ]
Powder | [pka]
15.57±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
LY2795050 is a short-acting selective κ(kappa)-opioid receptor (KOR) antagonist. LY2795050 has high affinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction[1][2]. | [in vivo]
LY2795050 (i.p., 0.032-0.1mg/kg, 30 min) prevents dose-dependent grooming deficits produced by U50,488 in male and female mice[2].
LY2795050 (i.p., 0.032-0.1mg/kg, 0-150 min) has sexual dimorphism in some behavioral effects[2]. | Animal Model: | C57BL/6J mice[2]
(gonadally intact, adult, male and female)
| | Dosage: | 0.032-0.1 mg/kg | | Administration: | i.p., 0.032-0.1mg/kg, 30 min | | Result: | Could dose-dependently prevent the self-grooming deficits caused by U50,488 with a 30-min pre-treatment.
Not effected in blocking the effects of U50,488 with smaller dose (0.032mg/kg) in either males or females.
Decreased immobility in the FST in males at a dose of 0.1mg/kg, but not in females, up to a dose of 0.32mg/kg.
Prevented and also reversed (at 0.32mg/kg) the locomotor-depressant effects of U50,488 (10mg/kg), in males and females.
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| [References]
[1] Ming-Qiang Zheng, et al. Synthesis and evaluation of 11C-LY2795050 as a κ-opioid receptor antagonist radiotracer for PET imaging. J Nucl Med DOI:10.2967/jnumed.112.109512
[2] Eduardo R Butelman, et al. Profile of a short-acting κ-antagonist, LY2795050, on self-grooming behaviors, forced swim test and locomotor activity: sex comparison in mice. J Psychopharmacol. 2021 May;35(5):579-590. DOI:10.1177/0269881121996883 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|