Nitenpyram-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENitenpyramCat. No.: HY-B0820CAS No.: 150824-47-8分式: CHClNO分量: 270.72作靶点: nAChR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解

2、性数据体外实验 DMSO : 250 mg/mL (923.46 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.6939 mL 18.4693 mL 36.9385 mL5 mM 0.7388 mL 3.6939 mL 7.3877 mL10 mM 0.3694 mL 1.8469 mL 3.6939 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证

3、实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.68 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (7.68 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90%

4、 corn oilSolubility: 2.08 mg/mL (7.68 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Nitenpyram类新烟碱和昆烟碱型酰胆碱受体 (nAChR) 激动剂，IC50 为 14 nM。Nitenpyram种服速效杀剂，于抑制猫狗等动物上的吮吸昆。体内研究 Nitenpyram is administered orally (1 mg/kg) for the short-term control of fleas in do

5、gs and cats. Fleas start tofall from the animals 30 minutes post-administration and one dose can protect animals for 1-2 days 1.Since Nitenpyram is highly lipophilic, it is administered orally after the meal in order to induce bile flow to helpdissolve the chemical, thereby increasing GI absorption

6、of the drug. It is rapidly and completely absorbedfrom the GI tract in less than 90 minutes and is completely excreted in urine within 48 hours after oraladministration to dogs and cats. Nitenpyram undergoes hydroxylation, followed by conjugation in the liver.The conjugates of Nitenpyram are excrete

7、d in the urine and Nitenpyram is not accumulated in body tissues.The plasma half-life of Nitenpyram in dogs and cats are 3 and 8 hours, respectively. It is likely that animalswith liver and/or kidney problems may have longer plasma half-life of Nitenpyram 1.REFERENCES1. Vo DT, et al. Insect nicotini

8、c acetylcholine receptor agonists as flea adulticides in small animals. J Vet Pharmacol Ther. 2010Aug;33(4):315-22.2. Rust MK, et al. Efficacy and longevity of nitenpyram against adult cat fleas (Siphonaptera: Pulicidae). J Med Entomol. 2003Sep;40(5):678-81.McePdfHeightCaution: Product has not been fully validated for medical applications.F