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MedKoo Cat#: 531410 | Name: AFDX384
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AFDX384 is potent M2/M4 selective antagonist.

Chemical Structure

AFDX384
CAS#118290-27-0

Theoretical Analysis

MedKoo Cat#: 531410

Name: AFDX384

CAS#: 118290-27-0

Chemical Formula: C27H38N6O2

Exact Mass: 478.3056

Molecular Weight: 478.64

Elemental Analysis: C, 67.75; H, 8.00; N, 17.56; O, 6.69

Price and Availability

Size Price Availability Quantity
10mg USD 450.00 2 Weeks
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Related CAS #
No Data
Synonym
AFDX384; AFDX 384; AFDX-384.
IUPAC/Chemical Name
N-[2-[2-[(dipropylamino)methyl]piperidin-1-yl]ethyl]-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide
InChi Key
MZDYABXXPZNUCT-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H38N6O2/c1-3-16-31(17-4-2)20-21-10-7-8-18-32(21)19-15-29-27(35)33-24-13-6-5-11-22(24)26(34)30-23-12-9-14-28-25(23)33/h5-6,9,11-14,21H,3-4,7-8,10,15-20H2,1-2H3,(H,29,35)(H,30,34)
SMILES Code
O=C(N1C2=NC=CC=C2NC(C3=CC=CC=C31)=O)NCCN4C(CN(CCC)CCC)CCCC4
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 478.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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PMID: 15652996. 5: Terry AV Jr, Hernandez CM, Hohnadel EJ, Bouchard KP, Buccafusco JJ. Cotinine, a neuroactive metabolite of nicotine: potential for treating disorders of impaired cognition. CNS Drug Rev. 2005 Autumn;11(3):229-52. doi: 10.1111/j.1527-3458.2005.tb00045.x. PMID: 16389292; PMCID: PMC6741756. 6: Pittel Z, Lazar S, Gez R, Chapman S. Early changes in M2 muscarinic acetylcholine receptors (mAChRs) induced by sarin intoxication may be linked to long lasting neurological effects. Neurotoxicology. 2018 Mar;65:248-254. doi: 10.1016/j.neuro.2017.11.002. Epub 2017 Nov 8. PMID: 29128314. 7: Croy CH, Chan WY, Castetter AM, Watt ML, Quets AT, Felder CC. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. doi: 10.1016/j.ejphar.2016.04.022. Epub 2016 Apr 13. PMID: 27085897. 8: Vaucher E, Reymond I, Najaffe R, Kar S, Quirion R, Miller MM, Franklin KB. Estrogen effects on object memory and cholinergic receptors in young and old female mice. Neurobiol Aging. 2002 Jan-Feb;23(1):87-95. doi: 10.1016/s0197-4580(01)00250-0. PMID: 11755023. 9: Sugawara S, Nakaya Y, Matsumura S, Hirose K, Saito Y, Kaneko R, Kobayashi M. Neural Subtype-dependent Cholinergic Modulation of Neural Activities by Activation of Muscarinic 2 Receptors and G Protein-activated Inwardly Rectifying Potassium Channel in Rat Periaqueductal Gray Neurons. Neuroscience. 2022 Dec 1;506:1-13. doi: 10.1016/j.neuroscience.2022.10.012. Epub 2022 Oct 18. PMID: 36270414. 10: DeAngelis MM, Hayes RL, Lyeth BG. Traumatic brain injury causes a decrease in M2 muscarinic cholinergic receptor binding in the rat brain. Brain Res. 1994 Aug 8;653(1-2):39-44. doi: 10.1016/0006-8993(94)90369-7. PMID: 7982073. 11: Hirose K, Nakaya Y, Kitano K, Saito Y, Kaneko R, Yanagawa Y, Yamamoto K, Shirakawa T, Kobayashi M. Differential regulation of medium spiny and cholinergic neurons in the nucleus accumbens core by the insular and medial prefrontal cortices in the rat. Pflugers Arch. 2021 Dec;473(12):1911-1924. doi: 10.1007/s00424-021-02634-y. Epub 2021 Nov 1. PMID: 34724104. 12: Mulugeta E, Karlsson E, Islam A, Kalaria R, Mangat H, Winblad B, Adem A. Loss of muscarinic M4 receptors in hippocampus of Alzheimer patients. Brain Res. 2003 Jan 17;960(1-2):259-62. doi: 10.1016/s0006-8993(02)03542-4. PMID: 12505680. 13: Grailhe R, Cardona A, Even N, Seif I, Changeux JP, Cloëz-Tayarani I. Regional changes in the cholinergic system in mice lacking monoamine oxidase A. Brain Res Bull. 2009 Mar 30;78(6):283-9. doi: 10.1016/j.brainresbull.2008.12.004. Epub 2008 Dec 25. PMID: 19111597. 14: Zavitsanou K, Nguyen VH, Han M, Huang XF. Effects of typical and atypical antipsychotic drugs on rat brain muscarinic receptors. Neurochem Res. 2007 Mar;32(3):525-32. doi: 10.1007/s11064-006-9266-9. PMID: 17268842. 15: Nieves-Martinez E, Haynes K, Childers SR, Sonntag WE, Nicolle MM. Muscarinic receptor/G-protein coupling is reduced in the dorsomedial striatum of cognitively impaired aged rats. Behav Brain Res. 2012 Feb 1;227(1):258-64. doi: 10.1016/j.bbr.2011.10.048. Epub 2011 Nov 7. PMID: 22085876; PMCID: PMC3253526. 16: Kitazawa T, Hirama R, Masunaga K, Nakamura T, Asakawa K, Cao J, Teraoka H, Unno T, Komori S, Yamada M, Wess J, Taneike T. Muscarinic receptor subtypes involved in carbachol-induced contraction of mouse uterine smooth muscle. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377(4-6):503-13. doi: 10.1007/s00210-007-0223-1. Epub 2007 Dec 11. PMID: 18071676. 17: Deng C, Weston-Green KL, Han M, Huang XF. Olanzapine treatment decreases the density of muscarinic M2 receptors in the dorsal vagal complex of rats. Prog Neuropsychopharmacol Biol Psychiatry. 2007 May 9;31(4):915-20. doi: 10.1016/j.pnpbp.2007.02.009. Epub 2007 Feb 20. PMID: 17368684. 18: Basu N, Scheuhammer AM, Rouvinen-Watt K, Evans RD, Grochowina N, Chan LH. The effects of mercury on muscarinic cholinergic receptor subtypes (M1 and M2) in captive mink. Neurotoxicology. 2008 Mar;29(2):328-34. doi: 10.1016/j.neuro.2008.01.003. Epub 2008 Jan 19. PMID: 18295336. 19: Nakamura T, Kimura J, Yamaguchi O. Muscarinic M2 receptors inhibit Ca2+-activated K+ channels in rat bladder smooth muscle. Int J Urol. 2002 Dec;9(12):689-96. doi: 10.1046/j.1442-2042.2002.00548.x. PMID: 12492954. 20: Bonsi P, Martella G, Cuomo D, Platania P, Sciamanna G, Bernardi G, Wess J, Pisani A. Loss of muscarinic autoreceptor function impairs long-term depression but not long-term potentiation in the striatum. J Neurosci. 2008 Jun 11;28(24):6258-63. doi: 10.1523/JNEUROSCI.1678-08.2008. PMID: 18550768; PMCID: PMC3849426.

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