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BIMU 8

Catalog No. T21946   CAS 134296-40-5

BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.

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BIMU 8 Chemical Structure
BIMU 8, CAS 134296-40-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 82.00
5 mg In stock $ 181.00
10 mg In stock $ 262.00
25 mg In stock $ 438.00
50 mg In stock $ 647.00
100 mg In stock $ 919.00
500 mg In stock $ 1,860.00
1 mL * 10 mM (in DMSO) In stock $ 195.00
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Purity: 99.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.
In vitro BIMU 8 (0.003-0.1 µM) increases excitatory postsynaptic potentials amplitude without changing the membrane potential of any neuron in myenteric neurons of guinea pig ileum[1].
In vivo BIMU 8 (20-30 mg/kg s.c. and 60 mg/kg p.o. in mice; 20 mg/kg i.p. in rats), produces significant antinociception. In mice, BIMU 8 (10 μg; i.c.v) which is largely ineffective by parenteral routes induces antinociception[2].
Molecular Weight 378.9
Formula C19H27ClN4O2
CAS No. 134296-40-5

Storage

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

Solubility Information

DMSO: 45 mg/mL (118.76 mM)

TargetMolReferences and Literature

1. H Pan , et al. 5-HT1A and 5-HT4 receptors mediate inhibition and facilitation of fast synaptic transmission in enteric neurons. Am J Physiol. 1994 Feb;266(2 Pt 1):G230-8. 2. C Ghelardini, et al. Central cholinergic antinociception induced by 5HT4 agonists: BIMU 1 and BIMU 8. Life Sci. 1996;58(25):2297-309. 3. Lucie P Pellissier, et al. Conformational toggle switches implicated in basal constitutive and agonist-induced activated states of 5-hydroxytryptamine-4 receptors. Mol Pharmacol. 2009 Apr;75(4):982-90.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library GPCR Compound Library Antidepressant Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

BIMU 8 134296-40-5 GPCR/G Protein Neuroscience 5-HT Receptor inhibit 5-hydroxytryptamine Receptor BIMU-8 Inhibitor antidepressant Serotonin Receptor BIMU8 antinociception 5-HT4 EPSP inhibitor

 

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