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VU0357017 hydrochloride

Cat. No. M5194
VU0357017 hydrochloride Structure
Synonym:

VU0357017 HCl

Size Price Availability Quantity
5mg USD 78.3  USD87 In stock
10mg USD 134.1  USD149 In stock
50mg USD 494.1  USD549 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

VU0357017 hydrochloride is a highly selective M1 agonist. VU0357017 hydrochloride acts at an allosteric site to activate the receptor. Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively. VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 HCl induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 HCl enhances performance in Morris water maze and contextual fear conditioning in rats.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 369.89
Formula C18H28ClN3O3
CAS Number 1135242-13-5
Purity >99%
Solubility DMSO 24 mg/mL
Storage at -20°C
References

Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.
Digby GJ, et al. ACS Chem Neurosci. 2012 Dec 19;3(12):1025-36. PMID: 23259038.

Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models.
Digby GJ, et al. J Neurosci. 2012 Jun 20;32(25):8532-44. PMID: 22723693.

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.
Lebois EP, et al. ACS Chem Neurosci. 2010;1(2):104-121. PMID: 21961051.

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  Catalog
Abmole Inhibitor Catalog 2017




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