Ibipinabant
Based on 1 publication(s) in Google Scholar
Ibipinabant (SLV319) is a potent, selective and orally active antagonist of cannabinoid CB1 receptor, with a Ki of 7.8 nM. Ibipinabant shows more than 1000-fold selectivity for CB1 over CB2 (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic.
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- Pureza: 99.90%
- No. CAS: 464213-10-3
- Fòrmula: C23H20Cl2N4O2S
- Peso molecular:487.40
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Ibipinabant
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Actividad biológica
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CB1 7.8 nM (Ki) |
CB2 7943 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1100 nM
Compound: SLV-319
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Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells
Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells
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[PMID: 17181138] |
| CHO | IC50 |
17 nM
Compound: SLV-319
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Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells
Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells
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[PMID: 17181138] |
SLV319 displaces the specific CP-55940 (CB agonist) binding in CHO cells stably transfected with human CB1 receptor, with a Ki of 7.8 nM[1].
SLV319 concentration dependently antagonizes WIN-55212 (CB1 agonist)-induced arachidonic acid release in CHO cells, with a pA2 of 9.9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SLV319 (3 mg/kg/day, p.o. for 28 d) reverses the HFD-induced increase in adipose tissue leptin mRNA[2].
SLV319 (3-10 mg/kg; daily oral gavage for 56 d) has weight loss-independent antidiabetic effects and attenuates β-cell loss in a rat model of progressive β-cell dysfunction[3].
SLV319 (oral administration) antagonizes CB agonist (CP55940) induced hypotension in rats and hypothermia in mice, with an ED50 of 5.5 and 3 mg/kg, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male C57Bl/6J mice received a diet containing 60% of calories as fat, resulting in body weights >42 g in 12-14 weeks[2]
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Dosage:3 mg/kg/day
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Administration:P.o. for 28 days
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Result:Caused reductions in food intake, body weight and adiposity in DIO mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 464213-10-3
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Appearance Solid
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Peso molecular 487.40
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Fòrmula C23H20Cl2N4O2S
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Color White to off-white
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SMILES
C/N=C(N1N=C(C2=CC=C(Cl)C=C2)[C@@H](C3=CC=CC=C3)C1)\NS(=O)(C4=CC=C(Cl)C=C4)=O
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Synonyms
SLV319; BMS-646256
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Bio Med Chem Au
Iso-α-acids in Nonalcoholic and Alcoholic Beer Stimulate Growth of Neuron-like SH-SY5Y Cells and Neuroepithelial Stem Cells. [Abstract]2021 Sep 7;1(1):11-20. PMID: 37101982
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lange JHM, et, al. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists. J Med Chem. 2004 Jan 29;47(3):627-43. [Content Brief]
[2]. Tam J, et, al. Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metab. 2012 Aug 8;16(2):167-79. [Content Brief]
[3]. Rohrbach K, et, al. Ibipinabant attenuates β-cell loss in male Zucker diabetic fatty rats independently of its effects on body weight. Diabetes Obes Metab. 2012 Jun;14(6):555-64. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ibipinabant Related Classifications
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