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CTEP (RO4956371) 97%

CTEP (RO4956371)

源葉(MedMol)
S81042
871362-31-1
C19H13ClF3N3O
391.77
品牌 貨號 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫存（上海） 北京 武漢 南京 購買數(shù)量
源葉(MedMol) S81042-1mg 97% ￥280.00元 10 - - -
源葉(MedMol) S81042-5mg 97% ￥722.50元 6 - - -
源葉(MedMol) S81042-10mg 97% ￥1275.00元 6 - - -
源葉(MedMol) S81042-25mg 97% ￥2700.00元 6 - - -
源葉(MedMol) S81042-50mg 97% ￥4700.00元 預(yù)計(jì)交期：2-3天 - - -
源葉(MedMol) S81042-100mg 97% ￥6600.00元 預(yù)計(jì)交期：2-3天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
產(chǎn)品描述： CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
靶點(diǎn)： mGlu5 Receptor:2.2 nM (IC50);GluR
體內(nèi)研究：
CTEP (RO 4956371) is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP (RO 4956371) significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in the Vogel conflict drinking test in rat, whereas it has no effect at lower doses. The half-life of CTEP (RO 4956371) (oral) is 18 h, and the B/P ratio based on total drug concentrations in plasma and whole brain homogenates is 2.6 in mice. After single oral doses of 4.5 and 8.7 mg/kg CTEP (RO 4956371) formulated as microsuspension in a saline/Tween vehicle administrated to adult C57BL/6 mice is rapidly absorbed and achieves close to maximal exposure after approximately 30 min. Chronic administration in adult mice with a dose of 2 mg/kg p.o. every 48 h for 2 months reaches a minimal CTEP (RO 4956371) brain exposure of 240 ng/g. CTEP (RO 4956371) fully displaces [3H]ABP688 in mouse brain regions known to express mGlu5, and 50% displacement is achieved with doses producing an average compound concentration of 77.5 ng/g measured in whole brain homogenate. CTEP (RO 4956371) (2 mg/kg, p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (RO 4956371) (2 mg/kg, p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse
參考文獻(xiàn)：
1. Lindemann L, et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J Pharmacol Exp Ther. 2011 Nov;339(2):474-86. 2. Michalon A, et al. Chronic pharmacological mGlu5 inhibition corrects fragile X in adult mice. Neuron. 2012 Apr 12;74(1):49-56.
溶解性： DMSO  :  ≥  100  mg/mL  (255.25  mM)
保存條件： -20℃
配置溶液濃度參考：
1mg 5mg 10mg
1 mM 2.553 ml 12.763 ml 25.525 ml
5 mM 0.511 ml 2.553 ml 5.105 ml
10 mM 0.255 ml 1.276 ml 2.553 ml
50 mM 0.051 ml 0.255 ml 0.511 ml
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