WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 530584
CAS#: Unknown (4/23/2017)
Description: AM-0466 is a potent and selective NaV1.7 Inhibitor (Nav 1.7 IC50 = 21 nM; Nav 1.5 IC50 =>30.0 uM. PXR = 22% @10 uM; CYP 2C9 IC50 = 4.6 uM; CYP3A4 TDI IC50 =>50.0 uM.). AM-0466 Affords Robust in Vivo Activity. AM-0466 demonstrated robust pharmacodynamic activity in a NaV1.7-dependent model of histamine-induced pruritus (itch) and additionally in a capsaicin-induced nociception model of pain without any confounding effect in open-field activity.
MedKoo Cat#: 530584
CAS#: Unknown (4/23/2017)
Chemical Formula: C27H19F3N4O4S
Exact Mass: 552.1079
Molecular Weight: 552.5282
Elemental Analysis: C, 58.69; H, 3.47; F, 10.32; N, 10.14; O, 11.58; S, 5.80
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Synonym: AM-0466; AM 0466; AM0466.
IUPAC/Chemical Name: 1-(3-methoxy-2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-2-oxo-N-(pyrimidin-2-yl)-1,2-dihydroquinoline-6-sulfonamide
InChi Key: RUFNTHMLMHZGFI-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H19F3N4O4S/c1-38-24-16-17(20-5-2-3-6-21(20)27(28,29)30)7-10-23(24)34-22-11-9-19(15-18(22)8-12-25(34)35)39(36,37)33-26-31-13-4-14-32-26/h2-16H,1H3,(H,31,32,33)
SMILES Code: O=S(NC1=NC=CC=N1)(C2=CC=C(N(C3=CC=C(C4=CC=CC=C4C(F)(F)F)C=C3OC)C(C=C5)=O)C5=C2)=O
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
The following data is based on the product molecular weight 552.5282 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.
|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|
1: Graceffa RF, Boezio AA, Able J, Altmann S, Berry LM, Boezio C, Butler JR,
Chu-Moyer M, Cooke M, DiMauro EF, Dineen TA, Feric Bojic E, Foti RS, Fremeau RT
Jr, Guzman-Perez A, Gao H, Gunaydin H, Huang H, Huang L, Ilch C, Jarosh M,
Kornecook T, Kreiman CR, La DS, Ligutti J, Milgram BC, Lin MJ, Marx IE, Nguyen
HN, Peterson EA, Rescourio G, Roberts J, Schenkel L, Shimanovich R, Sparling BA,
Stellwagen J, Taborn K, Vaida KR, Wang J, Yeoman J, Yu V, Zhu D, Moyer BD, Weiss
MM. Sulfonamides as Selective Na(V)1.7 Inhibitors: Optimizing Potency,
Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone
(AM-0466) that Affords Robust in Vivo Activity. J Med Chem. 2017 Apr 20. doi:
10.1021/acs.jmedchem.6b01850. [Epub ahead of print] PubMed PMID: 28324649.
Approximately 2% of the world’s population is affected by neuropathic pain.2 In the United States alone, it was estimated that the costs attributed to pain were approximately $600 billion annually.3 Currently, treatments for pain include opioids, antidepressants, anticonvulsants, and analgesics, which are often used in combination. These therapeutic approaches have several shortcomings such as limited efficacy, unwanted side effects including sedation and coordination impairment, and possible addiction. Additionally, it is estimated that only 50% of the patients can obtain satisfactory relief with current therapies.