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My CartCAS：170098-38-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 170098-38-1 |
| Name | Alvimopan dihydrate |
| Molecular Formula | C25H36N2O6 |
| Molecular Weight | 460.56 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD26142939 |
| 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 |
| InChIKey | USPVLEIQIUNQGE-DBFLIVQGSA-N |
| InChI | InChI=1S/C25H32N2O4.2H2O/c1-18-16-27(12-11-25(18,2)21-9-6-10-22(28)14-21)17-20(24(31)26-15-23(29)30)13-19-7-4-3-5-8-19;;/h3-10,14,18,20,28H,11-13,15-17H2,1-2H3,(H,26,31)(H,29,30);2*1H2/t18-,20-,25+;;/m0../s1 |
| PubChem CID | 5488547 |
| Target Point | Opioid Receptor |
| Passage | GPCR & G Protein;Neuronal Signaling |
| Background | Alvimopan dihydrate is a potent, relatively nonselective opioid antagonist |
| Biological Activity | 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 | 1.7nM(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]. |
| Data Literature Source | [1] Goldina Ikezuagu Erowele. P T. 2008，33(10): 574，580-583. [2] DT Beattie. Clinical Medicine: Therapeutics. 2009，1: 199-213. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
是一种有效的、相对非选择性的opioid拮抗剂
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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