| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
SIB-1893 targets the mGlu5 receptor subtype with an IC50 of 0.3 µM at hmGlu5. It is highly selective, showing >100 µM at hmGlu1b, hmGlu2, hmGlu6, hmGlu7, and hmGlu8.
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|---|---|
| ln Vitro |
In vitro, SIB-1893 is a selective and noncompetitive antagonist for the mGlu5 receptor subtype with an IC50 of 0.3 µM. Its selectivity has been confirmed in binding and functional assays.
|
| ln Vivo |
In rats that are allowed to move around, (E)-SIB-1893 causes hypothermia in a dose-dependent manner [1].
In vivo, (E)-SIB-1893 produces hypothermia in freely moving rats in a dose-dependent manner. It is used in models of pain, epilepsy, addiction, and neurodegenerative diseases. |
| Enzyme Assay |
In vitro receptor binding assays for SIB-1893 are performed using membrane preparations from cells expressing human recombinant mGlu5 receptors. Radioligand binding studies with [³H]MPEP or other mGlu5 ligands are used to determine the compound's binding affinity (Ki) and selectivity.
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| Cell Assay |
In vitro cellular assays for SIB-1893 measure its functional antagonism at mGlu5 receptors. Cells expressing the receptor are pre-treated with the compound and then stimulated with a mGlu5 agonist (e.g., glutamate or DHPG). The compound's ability to inhibit agonist-induced calcium mobilization or other downstream signaling is measured to determine its antagonist potency (IC50).
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| Animal Protocol |
In vivo animal studies with SIB-1893 are conducted in rodent models of pain, epilepsy, addiction, and neurodegenerative diseases. The compound is administered systemically, and behavioral responses are scored. For example, in models of neuropathic pain, the compound's ability to reduce pain responses is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for SIB-1893 are not detailed in publicly available sources. As a tool compound for in vivo studies, it is designed to have adequate brain penetration. Its PK properties would be characterized in preclinical species.
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| Toxicity/Toxicokinetics |
Toxicological data for SIB-1893 are not widely published. As a research compound, its safety profile is evaluated in the context of specific experiments. No significant toxicity has been reported in the available literature.
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| References | |
| Additional Infomation |
2-Methyl-6-(2-phenylvinyl)pyridine is a type of styrene compound.
SIB-1893 is a research compound and a highly selective, noncompetitive antagonist of the mGlu5 receptor. It is used as a tool to study the role of mGlu5 in various neurological and psychiatric disorders. It is not an approved drug. It exists as a racemate of (E)- and (Z)-isomers. |
| Molecular Formula |
C14H13N
|
|---|---|
| Molecular Weight |
195.26
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| Exact Mass |
195.105
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| CAS # |
6266-99-5
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| PubChem CID |
5311432
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| Appearance |
White to off-white solid powder
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| Density |
1.072g/cm3
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| Boiling Point |
307.3ºC at 760mmHg
|
| Flash Point |
128.8ºC
|
| Index of Refraction |
1.651
|
| LogP |
3.56
|
| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
|
| Complexity |
203
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=NC(=CC=C1)/C=C/C2=CC=CC=C2
|
| InChi Key |
SISOFUCTXZKSOQ-ZHACJKMWSA-N
|
| InChi Code |
InChI=1S/C14H13N/c1-12-6-5-9-14(15-12)11-10-13-7-3-2-4-8-13/h2-11H,1H3/b11-10+
|
| Chemical Name |
2-methyl-6-[(E)-2-phenylethenyl]pyridine
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| Synonyms |
SIB1893; SIB 1893; SIB-1893
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~512.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.1214 mL | 25.6069 mL | 51.2138 mL | |
| 5 mM | 1.0243 mL | 5.1214 mL | 10.2428 mL | |
| 10 mM | 0.5121 mL | 2.5607 mL | 5.1214 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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