WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 526876
Description: AM-2099 is a potent and selective NaV1.7 Inhibitor (hNav1.7 IC50 = 0.16 uM; hNav1.5 IC50 > 30 uM; Papp = 31 x 10 (-6)cm/s; Rat IV CL (b/h/kg) \= 0.54; cLogD = 2.1). AM-2099 demonstrated a favorable pharmacokinetic profile in rat and dog and demonstrated dose-dependent reduction of histamine-induced scratching bouts in a mouse behavioral model following oral dosing.
MedKoo Cat#: 526876
Chemical Formula: C19H13F3N4O3S2
Exact Mass: 466.0381
Molecular Weight: 466.4532
Elemental Analysis: C, 48.92; H, 2.81; F, 12.22; N, 12.01; O, 10.29; S, 13.75
This product is not in stock, which may be available by custom synthesis.
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Synonym: AM-2099; AM2099; AM 2099.
IUPAC/Chemical Name: 4-(2-methoxy-4-(trifluoromethyl)phenyl)-N-(thiazol-2-yl)quinazoline-7-sulfonamide
InChi Key: VSUDRCZPHWUXEW-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H13F3N4O3S2/c1-29-16-8-11(19(20,21)22)2-4-14(16)17-13-5-3-12(9-15(13)24-10-25-17)31(27,28)26-18-23-6-7-30-18/h2-10H,1H3,(H,23,26)
SMILES Code: O=S(C1=CC=C2C(N=CN=C2C3=C(OC)C=C(C(F)(F)F)C=C3)=C1)(NC4=NC=CS4)=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 466.4532 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|
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement
Isaac E. Marx, Thomas A. Dineen, Jessica Able, Christiane Bode, Howard Bregman, Margaret Chu-Moyer, Erin F. DiMauro, Bingfan Du, Robert S. Foti, Robert T. Fremeau Jr., Hua Gao, Hakan Gunaydin, Brian E. Hall, Liyue Huang, Thomas Kornecook, Charles R. Kreiman, Daniel S. La, Joseph Ligutti, Min-Hwa Jasmine Lin, Dong Liu, Jeff S. McDermott, Bryan D. Moyer, Emily A. Peterson, Jonathan T. Roberts, Paul Rose, Jean Wang, Beth D. Youngblood, Violeta Yu, and Matthew M. Weiss
Publication Date (Web): September 21, 2016 (Letter)