SIB-1757
Based on 1 Customer Validation
SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC50 of 0.4 μM.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 31993-01-8
- Formula: C12H11N3O
- Molecular Weight:213.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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human mGluR5 0.4 μM (IC50) |
SIB-1757 (2 μM) reduces the 3,5-DHPG-induced membrane depolarization of the recorded neuron in striatal cholinergic interneurons[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SIB-1757 (intraplantar injection of 100 μg, or s.c. injection of 20 mg/kg) reverses spinal nerve ligation-induced thermal hyperalgesia in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 31993-01-8
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Appearance Solid
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Molecular Weight 213.24
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Formula C12H11N3O
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Color Orange to red
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SMILES
OC1=CC=C(C)N=C1/N=N/C2=CC=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 12.5 mg/mL (58.62 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 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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Handling Instructions (2659 KB)
References
[1]. Varney MA, et al. SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5. J Pharmacol Exp Ther. 1999 Jul;290(1):170-81. [Content Brief]
[2]. Storto M, et al. Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice. J Hepatol. 2003 Feb;38(2):179-87. [Content Brief]
[3]. Dogrul A, et al. Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR(5)) antagonist, in experimental neuropathic pain in rats. Neurosci Lett. 2000 Oct 6;292(2):115-8. [Content Brief]
[4]. Bonsi P, et al. Modulatory action of metabotropic glutamate receptor (mGluR) 5 on mGluR1 function in striatal cholinergic interneurons. Neuropharmacology. 2005;49 Suppl 1:104-13. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.6896 mL | 23.4478 mL | 46.8955 mL | 117.2388 mL |
| 5 mM | 0.9379 mL | 4.6896 mL | 9.3791 mL | 23.4478 mL | |
| 10 mM | 0.4690 mL | 2.3448 mL | 4.6896 mL | 11.7239 mL | |
| 15 mM | 0.3126 mL | 1.5632 mL | 3.1264 mL | 7.8159 mL | |
| 20 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8619 mL | |
| 25 mM | 0.1876 mL | 0.9379 mL | 1.8758 mL | 4.6896 mL | |
| 30 mM | 0.1563 mL | 0.7816 mL | 1.5632 mL | 3.9080 mL | |
| 40 mM | 0.1172 mL | 0.5862 mL | 1.1724 mL | 2.9310 mL | |
| 50 mM | 0.0938 mL | 0.4690 mL | 0.9379 mL | 2.3448 mL |
SIB-1757 Related Classifications
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