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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > AMG-517CAS：659730-32-2
Molecular Formula：C20H13F3N4O2S
Molecular Weight：430.4
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 659730-32-2 |
| Name | AMG-517 |
| Molecular Formula | C20H13F3N4O2S |
| Molecular Weight | 430.4 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD14584859 |
| SMILES | CC(NC1=NC2=C(OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)C=CC=C2S1)=O |
| Target Point | TRPV |
| Passage | Membrane Transporter&Ion Channel;Neuronal Signaling |
| Background | AMG-517 is a potent vanilloid receptor-1 (TRPV1) antagonist. |
| Biological Activity | AMG-517是一种有效的，选择性的TRPV1拮抗剂，抑制TRPV1的Capsaicin， Proton和热激活，IC50分别为0.76 nM， 0.62 nM和1.3 nM。[1-2] |
| In Vitro | AMG 517抑制 CAP-(500 nM)，酸(pH 5.0)，或热(45°C)诱导的45Ca2+流入人体表达TRPV1的CHO细胞，IC50分别为0.76 nM，0.62 nM 和 1.3 nM。AMG 517作用于表达TRPV1的细胞，抑制Capsaicin，Proton，和热诱导的内向电流。AMG 517作用于大鼠背根神经节神经元，抑制Capsaicin诱导的天然TRPV1激活，IC50值为0.68 nM。AMG 517是大鼠和人类TRPV1的竞争性拮抗剂，解离常数(Kb)分别为4.2 和6.2 nM。AMG 517是高度选择性的TRPV1拮抗剂。AMG 517作用于重组表达适当TRP通道的CHO细胞，作用于2-APB激活的TRPV2 和TRPV3，4-αPDD激活的 TRPV4，异硫氰酸烯丙酯激活TRPA1，和 Icilin激活的 TRPM8，IC50值>20 μM。[1] |
| In Vivo | AMG 517口服处理，导致血浆浓度增加，这种作用存在以剂量依赖性，也降低Capsaicin处理诱导的血块退缩数量，这种作用也存在剂量依赖性。根据对照组和Capsaicin实验组的退缩数量在统计上的显著差异，得出AMG 517的最低有效剂量(MED)为0.3 mg/kg。AMG 517的相应血浆浓度为90至100 ng/mL。AMG 517(3 mg/kg)处理24小时后，显著降低Capsaicin诱导的退缩。AMG 517作用于CFA疼痛模型，抑制热痛觉过敏。[1]AMG 517作用于啮齿类动物，狗和猴子，但不是TRPV1基因敲除的小鼠，引发体温过高。有趣的是，TRPV1选择性拮抗剂诱发的体温过高可通过重复给药大鼠，狗，和猴，及TRPV1基因敲除的小鼠这些拮抗剂得到衰减，体温不会出现降低。[2] |
| Cell Experiment | Animal Models: 雄性Sprague-Dawley大鼠; Dosages: 0.003-3 mg/kg; Administration: 口服处理[1] |
| Data Literature Source | [1] Gavva NR，et al. J Pharmacol Exp Ther，2007，323(1)，128-137. [2] Gavva NR，et al. Pain，2008，136(1-2)，202-210. |
| Unit | Bottle |
| Specification | 2mg 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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