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MedKoo Cat#: 530584 | Name: AM-0466

Description:

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

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.

Chemical Structure

AM-0466
AM-0466
CAS#Unknown (4/23/2017)

Theoretical Analysis

MedKoo Cat#: 530584

Name: AM-0466

CAS#: Unknown (4/23/2017)

Chemical Formula: C27H19F3N4O4S

Exact Mass: 552.1079

Molecular Weight: 552.53

Elemental Analysis: C, 58.69; H, 3.47; F, 10.32; N, 10.14; O, 11.58; S, 5.80

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
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
More Info
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.

Preparing Stock Solutions

The following data is based on the product molecular weight 552.53 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
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.