Timolol Maleate

马来酸噻吗心安,MK-950,MK 950,MK950

(S)-Timolol Maleate是非选择性β-肾上腺素受体拮抗剂,对β1和β2受体亚型的Ki分别为1.97和2.0 nM。

目录号
EY1428
EY1428
纯度
99.43%
99.43%
规格
100 mg
200 mg
原价
480
820
售价
480
820
库存
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Timolol Maleate is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with Ki of 1.97 nM/2.0 nM.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Hall RA, et al. Arch Int Pharmacodyn Ther, 1975, 213(2), 251-263.

    分子式
    C17H28N4O7S
    分子量
    432.49
    CAS号
    26921-17-5
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    85 mg/mL
    Water
    <1 mg/mL
    Ethanol
    85 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01607671 Optic Neuropathy, Ischemic|Anterior Ischemic Optic Neuropathy|Ischemic Optic Neuropathy|Optic Neuropathy, Anterior Ischemic Drug: Timolol maleate Fraser Health Phase 1 2012-06-01 2015-05-22
    NCT01685398 Hemangioma Drug: 0.5% timolol maleate eye drop|Drug: Normal saline Mahidol University Phase 3 2012-09-01 2012-11-26
    NCT02145884 Hemangioma Drug: timolol maleate 0.5% gel Rady Children's Hospital, San Diego|Valeant Pharmaceuticals Phase 2 2014-05-01 2017-02-09
    NCT02422017 Venous Leg Ulcers Drug: Timolol|Other: Local care treatment Centre Hospitalier Universitaire, Amiens Phase 2 2015-04-01 2016-11-29
    NCT01533376 Sturge Weber Syndrome|Port-wine Mark Drug: Timolol|Drug: Preservative free artificial tear gel. Wills Eye|University of Medicine and Dentistry of New Jersey Phase 1 2012-02-01 2015-12-18
    NCT02484716 Hemorrhagic Hereditary Telangiectasia (HHT) Drug: Timolol nasal spray|Drug: Placebo nasal spray Hospices Civils de Lyon Phase 2 2015-06-01 2016-11-08
    NCT02731287 Hemangioma Drug: Timolol|Drug: Placebo Fundaci贸 Institut de Recerca de l'Hospital de la Santa Creu i Sant Pau Phase 2 2014-03-01 2016-04-06
    NCT00735449 Glaucoma|Ocular Hypertension Drug: Fixed combination of brimonidine tartrate 0.2% timolol maleate 0.5%|Drug: timolol maleate 0.5%|Drug: latanoprost 0.005% Allergan Phase 4 2008-07-01 2012-11-13
    NCT02774590 Acne Vulgaris|Rosacea Drug: Timolol Johns Hopkins University Phase 1 2016-03-01 2016-05-12
    NCT00823043 Open-angle Glaucoma|Ocular Hypertension Drug: timolol hemihydrate|Drug: timolol maleate Vistakon Pharmaceuticals 2009-01-01 2015-02-18
    NCT01749904 Open-Angle Glaucoma|Ocular Hypertension Drug: BOL-303259-X|Drug: Timolol|Drug: BOL-303259-X Bausch & Lomb Incorporated Phase 3 2013-01-01 2015-11-10
    NCT01749930 Open-Angle Glaucoma|Ocular Hypertension Drug: BOL-303259-X|Drug: Timolol|Drug: BOL-303259-X Bausch & Lomb Incorporated Phase 3 2013-01-01 2015-11-10
    NCT01707381 Ocular Hypertension|Open Angle Glaucoma Drug: BOL-303259-X|Drug: Timolol maleate Bausch & Lomb Incorporated Phase 2 2012-11-01 2014-11-24
    NCT01250457 Benign Vascular Periocular Lesions Drug: topical Timolol Loyola University Phase 4 2010-06-01 2012-10-29
    NCT01147601 Hemangioma|Infant Drug: topical 0.5% Timolol|Drug: Control (placebo) group Oregon Health and Science University Early Phase 1 2010-03-01 2010-06-18
    NCT00757835 Glaucoma Drug: treatment with latanoprost/timolol fixed combination|Drug: latanoprost/timolol fixed combination drops Aristotle University Of Thessaloniki|Alcon Research Phase 4 2008-05-01 2014-05-09
    NCT00972257 Glaucoma Drug: treatment with dorzolamide/timolol|Drug: treatment with brimonidine/timolol Aristotle University Of Thessaloniki Phase 4 2009-01-01 2014-05-09
    NCT02214680 Healthy Drug: Combigan (Combination of Brimonidine and Timolol)|Drug: Timolol Carmel Medical Center Phase 2 2015-10-01 2015-10-13
    NCT01408056 Infantile Hemangiomas Drug: Timolol 0.5% Gel Forming Solution (GFS)|Drug: Mupirocin 2% Ointment Children's Hospital of Philadelphia|Society for Pediatric Dermatology Phase 2 2011-02-01 2014-01-16
    NCT00832377 Glaucoma Drug: timolol/dorzolamide combination Merck Sharp & Dohme Corp. Phase 2 2009-04-01 2015-02-06

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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