GSK1059865
Modify Date: 2024-03-11 10:48:44
GSK1059865 structure
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Common Name | GSK1059865 | ||
|---|---|---|---|---|
| CAS Number | 1191044-58-2 | Molecular Weight | 436.318 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 575.8±50.0 °C at 760 mmHg | |
| Molecular Formula | C20H23BrFN3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 302.1±30.1 °C | |
Use of GSK1059865GSK1059865 is a potent orexin 1 receptor antagonist. |
| Name | GSK1059865 |
|---|---|
| Synonym | More Synonyms |
| Description | GSK1059865 is a potent orexin 1 receptor antagonist. |
|---|---|
| Related Catalog | |
| Target |
Orexin 1 receptor[1] |
| In Vivo | Treatment with GSK1059865 significantly decreases ethanol drinking in a dose-dependent manner in CIE-exposed mice. In contrast GSK1059865 decreases drinking in air-exposed mice only at the highest dose used. There is no effect of GSK1059865 on sucrose intake[1]. GSK1059865 (0.3 nM-10 nM) produces non-surmountable antagonism with a dose-dependent rightward shift of the OXA EC50 and a concomitant decrease of the agonist maximal response. The calculated pKB value is 8.77±0.12 for GSK1059865. GSK1059865 (0.1-3.3 μM) produces a classical surmountable profile with parallel rightward shift of the OXA EC50 without depression of the agonist maximal response[2]. Intraperitoneal administration of GSK1059865 produces a region-dependent inhibition of yohimbine-induced relative cerebral blood volume response. The administration of GSK1059865 per se produces a weak relative cerebral blood volume increase in several brain regions. GSK1059865-pretreated animals exhibit slightly higher baseline mean arterial blood pressure values than controls[3]. |
| Animal Admin | Rats: GSK1059865 is dissolved in 0.5% HPMC (w/v) in distilled water and administered by gavage at doses of 10 and 30 mg/kg to rats. Drug or vehicle is administered 1 h before access to highly palatable food[2]. Mice: During baseline and the first 5 test cycles following chronic intermittent ethanol (or air) exposure, mice receive vehicle (saline) injections (i.p.; 0.01 ml/g body weight) 30 minutes before drinking ethanol. On test cycles 6 and 7 mice receive vehicle or GSK1059865 (10, 25, 50 mg/kg) before given access to ethanol 15% v/v (Test 6) or sucrose 5% w/v (Test 7) versus water. GSK1059865 is dissolved in saline and TWEEN 80 (0.5 % v/v) as vehicle[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 575.8±50.0 °C at 760 mmHg |
| Molecular Formula | C20H23BrFN3O2 |
| Molecular Weight | 436.318 |
| Flash Point | 302.1±30.1 °C |
| Exact Mass | 435.095764 |
| LogP | 4.41 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.592 |
| Storage condition | 2-8℃ |
| [(2S,5S)-2-{[(5-Bromo-2-pyridinyl)amino]methyl}-5-methyl-1-piperidinyl](3-fluoro-2-methoxyphenyl)methanone |
| Methanone, [(2S,5S)-2-[[(5-bromo-2-pyridinyl)amino]methyl]-5-methyl-1-piperidinyl](3-fluoro-2-methoxyphenyl)- |
- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: GSK1059865
- Price: Negotiable
- Purity: 99.0%
- Delivery: 10 Day
- Contact: Huang
- Email: sales@echemcloud.com
- DC Chemicals Limited
- China
- Product Name: GSK1059865
- Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
- Purity: 98.0%
- Delivery: 3 Day
- Contact: Tony Cao
- Email: sales@dcchemicals.com
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: GSK1059865
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Delivery: Inquiry
- Contact: Ms Wang
- Email: enquiry@dycnchem.com
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Price: $211/10mM*1mLinDMSO
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