| Identification | Back Directory | [Name]
AM-2099 | [CAS]
1443373-17-8 | [Synonyms]
AM-2099
AM 2099;AM-2099
4-[2-Methoxy-4-(trifluoromethyl)phenyl]-N-2-thiazolyl-7-quinazolinesulfonamide
7-Quinazolinesulfonamide, 4-[2-methoxy-4-(trifluoromethyl)phenyl]-N-2-thiazolyl- | [Molecular Formula]
C19H13F3N4O3S2 | [MDL Number]
MFCD30738047 | [MOL File]
1443373-17-8.mol | [Molecular Weight]
466.46 |
| Chemical Properties | Back Directory | [Boiling point ]
572.1±60.0 °C(Predicted) | [density ]
1.531±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 150 mg/mL (321.57 mM) | [form ]
Solid | [pka]
6.11±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. | [Uses]
AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7. | [in vivo]
AM-2099 demonstrates a favorable pharmacokinetic profile in rat and dog. In rats AM-2099 shows low total clearance and moderate Vdss and half-life. In contrast, when dosed in dogs AM-2099 shows very low clearance, a low Vdss and long halflife (18 h). AM-2099 demonstrates a dose-dependent increase in plasma exposure with a concomitant dose-dependent reduction in scratching bouts compared to vehicle-treated animals, with a statistically significant reduction observed at the 60 mg/kg dose[1]. | [IC 50]
Nav1.7 | [References]
[1] Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. DOI:10.1021/acsmedchemlett.6b00243 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|