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A1397250

AMG9810 , ≥99% , 545395-94-6

Synonym(s):
2E-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-Propenamide

CAS NO.:545395-94-6

Empirical Formula: C21H23NO3

Molecular Weight: 337.41

MDL number: MFCD00955103

Pack Size Price Stock Quantity
5mg RMB239.20 In Stock
10mg RMB342.40 In Stock
25mg RMB799.20 In Stock
50mg RMB1209.60 In Stock
100mg RMB2399.20 In Stock
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Update time: 2022-07-08

PRODUCT Properties

Boiling point: 512.5±50.0 °C(Predicted)
Density  1.175±0.06 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: >5mg/mL
pka 12.22±0.20(Predicted)
form  powder
color  white to beige
InChI 1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+
InChIKey GZTFUVZVLYUPRG-IZZDOVSWSA-N
SMILES CC(C)(C)c1ccc(\C=C\C(=O)Nc2ccc3OCCOc3c2)cc1

Description and Uses

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.

AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.[Cayman Chemical]

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H413
Precautionary statements  P264-P270-P273-P301+P312-P501
PPE dust mask type N95 (US), Eyeshields, Gloves
Hazard Codes  Xn
Risk Statements  22
WGK Germany  3
Storage Class 11 - Combustible Solids
Hazard Classifications Acute Tox. 4 Oral
Aquatic Chronic 4

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