Amg 517
- Product Name
- Amg 517
- CAS No.
- 659730-32-2
- Chemical Name
- Amg 517
- Synonyms
- CS-691;AM -517;Amg 517;AMG-517 ，S7115;AMG517; AMG-517;AMG 517, 10 mM in DMSO;N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide;AcetaMide, N-[4-[[6-[4-(trifluoroMethyl)phenyl]-4-pyriMidinyl]oxy]-2-benzothiazolyl]-;N-(4-((6-(4-(Trifluoromethyl)phenyl)pyrimidin-4-yl)oxy)benzo[d]thiazol-2-yl)acetamide;N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide AMG517
- CBNumber
- CB82516228
- Molecular Formula
- C20H13F3N4O2S
- Formula Weight
- 430.4
- MOL File
- 659730-32-2.mol
Amg 517 Property
- Melting point:
- 227℃
- Density
- 1.458
- storage temp.
- Store at -20°C
- solubility
- ≥21.5 mg/mL in DMSO; insoluble in H2O; ≥4.93 mg/mL in EtOH
- form
- solid
- pka
- 10.19±0.70(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 26191
- Product name
- AMG 517
- Packaging
- 5mg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 26191
- Product name
- AMG 517
- Packaging
- 10mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 26191
- Product name
- AMG 517
- Packaging
- 25mg
- Price
- $268
- Updated
- 2024/03/01
- Product number
- 26191
- Product name
- AMG 517
- Packaging
- 50mg
- Price
- $469
- Updated
- 2024/03/01
- Product number
- 5995
- Product name
- AMG517
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $193
- Updated
- 2021/12/16
Amg 517 Chemical Properties,Usage,Production
Uses
AMG-517 is a novel TRPV1 antagonist.
Biological Activity
AMG517 is an orally active, highly potent and selective vanilloid receptor-1 (TRPV1; VR1; capsaicin receptor) antagonist th at blocks TRPV1-mediated cellular Ca2+ influx (h/r/m IC50/stimulant = 0.76 nM/1.01 nM/1.9 nM/500 nM capsaicin; 0.62 nM/0.5 nM/0.63 nM/acid (pH 5) using respective CHO transfectants; IC50 >20 μM against TRPV2/3/4, TRPA1, and TRPM8-mediated responses; <45% binding at 10 μM to 87 receptors, enzymes, and ion channels) and exhibits antihyperalgesic efficacy in vivo (capsaicin-induced flinch = ED50 = 0.33 mg/kg rats, p.o.; CFA-induced thermal hyperalgesia, MED = 0.83 mg/kg rats, p.o.).
in vivo
AMG 517 is shown to be effective in a rodent "on-target" biochemical challenge model (capsaicin-induced flinch, ED50=0.33 mg/kg p.o.) and is antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED=0.83 mg/kg, p.o.)[1].The minimally effective dose is 0.3 mg/kg for AMG 517 and the corresponding plasma concentration is 90 ng/mL. Oral administration of AMG 517 reverses established thermal hyperalgesia in a dose-dependent manner at 21 h after CFA injection. AMG 517 causes transient hyperthermia in rodents, dogs, and monkeys. AMG 517 induces hyperthermia in a steep dose-dependent manner, with 0.3, 1, and 3 mg/kg associated with 0.5, 0.6, and 1.6°C increases in body temperature, respectively. Body temperatures of rats treated with all doses of AMG 517 return to baseline within 10 to 20 h[2].
storage
Store at +4°C
Amg 517 Preparation Products And Raw materials
Raw materials
Preparation Products
Amg 517 Suppliers
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