Alvimopan dihydrate/ADL 8-2698 dihydrate;爱维莫潘二水合物

Alvimopan dihydrate/ADL 8-2698 dihydrate;爱维莫潘二水合物

货号:
IA2140

品牌:
Jinpan

Alvimopan dihydrate/ADL 8-2698 dihydrate;爱维莫潘二水合物

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产品简介
MDL MFCD26142939
别名 ADL8-2698dihydrate;LY246736dihydrate
英文名称 Alvimopan dihydrate/ADL 8-2698 dihydrate
CAS 170098-38-1
分子式 C25H36N2O6
分子量 460.56
纯度 ≥98%
单位
生物活性 Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus[1-[3].
IC50 1.7 nM (μ-opioid receptor)[1]
In Vitro Alvimopan inhibits the loperamide-stimulated [35S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC50 of 1.7 nM[1].
In Vivo Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of 113Sn-labelled microspheres produced by morphine in rats.Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats[3].
SMILES OC1=CC=CC([C@@]2(C)[C@@H](C)CN(C[C@H](CC3=CC=CC=C3)C(NCC(O)=O)=O)CC2)=C1.O.O
靶点 Opioid Receptor
数据来源文献 [1] Goldina Ikezuagu Erowele. P T. 2008, 33(10): 574, 580-583.
[2] DT Beattie. Clinical Medicine: Therapeutics. 2009, 1: 199-213.
规格 5mg 10mg 50mg

是一种有效的、相对非选择性的opioid拮抗剂