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(E/Z)-SIB-1893

Catalog No. T23353 CAS 6266-99-5

Synonyms: SIB 1893

(E/Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity .

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(E/Z)-SIB-1893, CAS 6266-99-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 67.00
10 mg	In stock	$ 118.00
25 mg	In stock	$ 247.00
50 mg	In stock	$ 392.00
100 mg	In stock	$ 592.00
500 mg	In stock	$ 1,280.00

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Purity: 99.92%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	(E/Z)-SIB-1893 (SIB 1893) is the racemate of (E)-SIB-1893 and (Z)-SIB-1893. (E)-SIB-1893 is a selective, noncompetitive mGluR5 antagonist with anticonvulsant activity .
In vitro	We investigated the role of mGluR5 in acute NMDA and glutamate-mediated neurodegeneration in cultured rat cortical cells using the mGluR5 antagonists SIB-1893 (20 or 200 μM; rat cortical cells) and found that they provide significant protection.[4]
In vivo	SIB-1893 (10, 20, and 30 mg/kg; i.p.; 0-180 min) considerably lowered the body temperature in animals at 90, 120, and 180 min after its systemic injection of 30 mg/kg. In contrast, the drug at 10 and 20 mg/kg remained without effect on the body temperature in rats. Based on our preclinical study, one can conclude that SIB-1893 produces hypothermia in freely moving rats in a dose-dependent manner.[1] SIB 1893 (10 and 20 mg/kg; mice; i.p.) did not affect the protective action of valproate, ethosuximide, phenobarbital, and clonazepam in this test. The combined treatment of SIB 1893 with conventional antiepileptic drugs did not lead to motor impairment. Long-term memory disturbances were observed only in the case of the combination of SIB 1893 with phenobarbital.[2]

Synonyms	SIB 1893
Molecular Weight	195.26
Formula	C14H13N
CAS No.	6266-99-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (460.9 mM), Sonication is recommended.

References and Literature

1. Łuszczki JJ, et al. Non-competitive metabotropic glutamate subtype 5 receptor antagonist (SIB-1893) decreases body temperature in rats. Pharmacol Rep. 2005;57(6):795-801. 2. Borowicz KK, et al. Influence of SIB 1893, a selective mGluR5 receptor antagonist, on the anticonvulsant activity of conventional antiepileptic drugs in two models of experimental epilepsy. Pol J Pharmacol. 2003;55(5):735-740. 3. Storto M, et al. Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice. J Hepatol. 2003;38(2):179-187. 4. O'Leary DM, et al. Selective mGluR5 antagonists MPEP and SIB-1893 decrease NMDA or glutamate-mediated neuronal toxicity through actions that reflect NMDA receptor antagonism. Br J Pharmacol. 2000;131(7):1429-1437.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Bioactive Compound Library Neuronal Signaling Compound Library Bioactive Compounds Library Max

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Keywords

(E/Z)-SIB-1893 6266-99-5 Neuroscience Others GluR SIB 1893 (E/Z)-SIB1893 (E/Z)-SIB 1893 SIB1893 SIB-1893 inhibitor inhibit

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