Unoprostone
(Synonyms: 乌诺前列酮) 目录号 : GC41248A PGF2α analog
Cas No.:120373-36-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Unoprostone is an analog of PGF2α with a 13,14-dihydro-15-keto modification and a two-carbon extension of the aliphatic lower side chain. The isopropyl ester of unoprostone ( (Rescula) has been approved for clinical use as an ocular hypotensive drug.
| Cas No. | 120373-36-6 | SDF | |
| 别名 | 乌诺前列酮 | ||
| Canonical SMILES | O[C@@H]1[C@H](C/C=C\CCCC(O)=O)[C@@H](CCC(CCCCCCC)=O)[C@H](O)C1 | ||
| 分子式 | C22H38O5 | 分子量 | 382.5 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 17 mg/ml,Ethanol: 12 mg/ml,PBS (7.2): 90 µ g/ml | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6144 mL | 13.0719 mL | 26.1438 mL |
| 5 mM | 0.5229 mL | 2.6144 mL | 5.2288 mL |
| 10 mM | 0.2614 mL | 1.3072 mL | 2.6144 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Current status of Unoprostone for the management of glaucoma and the future of its use in the treatment of retinal disease
Expert Opin Pharmacother 2013 Jan;14(1):105-13.PMID:23199345DOI:10.1517/14656566.2013.748038.
Introduction: Optic nerve and retinal diseases such as glaucoma, age-related macular degeneration (AMD) and retinitis pigmentosa (RP) are significant public health concerns and have a momentous impact on patients' functional status and quality of life. These diseases are among the most common causes of visual impairment worldwide and account for billions of dollars in healthcare expenditures and lost productivity. The importance of adequate treatment of these conditions and the need for efficacious therapeutic drugs cannot be overstated. Unoprostone continues to be developed as a potential treatment for these debilitating diseases. Areas covered: This review provides background information on Unoprostone isopropyl (Unoprostone), a prostanoid and synthetic docosanoid approved for the treatment of open-angle glaucoma and ocular hypertension, and recapitulates safety and efficacy data as it relates to this indication. Additionally, this review describes potential new uses of Unoprostone as therapy for dry AMD and RP. A literature search of peer-reviewed publications was performed utilizing PubMed. Searches were last updated on 10 September 2012. Expert opinion: Current data indicate that Unoprostone does significantly lower intraocular pressure (IOP) and has a favorable safety and tolerability profile. However, the IOP-lowering effects of Unoprostone do not compare with other commercially available prostanoids and it has the disadvantage of a twice-daily rather than once-daily dosing regimen. Nonetheless, recent data suggest that Unoprostone may improve neuronal survival and increase ocular blood flow, indicating that it may have some value as a therapy for glaucoma, RP and dry AMD. Further studies are needed to confirm whether Unoprostone provides any clinically significant advantage over the other commercially available prostanoids.
Unoprostone (isopropyl Unoprostone)
Drugs Aging 1996 Sep;9(3):213-8; discussion 219-20.PMID:8877315DOI:10.2165/00002512-199609030-00007.
Unoprostone (isopropyl Unoprostone) is a docosanoid compound which is related to a metabolite of prostaglandin (PG)F2 alpha. Unoprostone has oculo-hypotensive effects. The drug is thought to lower intraocular pressure (IOP) by increasing aqueous humour outflow. Aqueous humour production remains unaffected. Marked reductions in IOP have been demonstrated in healthy volunteers and patients with glaucoma or ocular hypertension after instillation of Unoprostone 0.12%. Unoprostone 0.12% appears to have similar efficacy to timolol 0.5% in patients with primary open-angle glaucoma or ocular hypertension. In phase II and III clinical studies, adverse events observed with Unoprostone were predominantly local; systemic effects occurred less frequently.
Safety of Unoprostone isopropyl as mono- or adjunctive therapy in patients with primary open-angle glaucoma or ocular hypertension
Drug Saf 2002;25(8):583-97.PMID:12113643DOI:10.2165/00002018-200225080-00004.
This review summarises the safety of Unoprostone isopropyl (both at the 0.12 and 0.15% concentrations) instilled twice daily in patients with primary open-angle glaucoma (POAG) or ocular hypertension (OH). For Unoprostone 0.15%, combined data from two 12-month comparative monotherapy studies are reported, as well as data from three adjunctive therapy studies and two special population studies. With Unoprostone monotherapy, most adverse events were mild or moderate and transient in nature. Less than 7% of unoprostone-treated patients discontinued therapy due to an adverse event. The most common adverse events associated with Unoprostone were burning/stinging, burning/stinging directly upon drug instillation, ocular itching, and conjunctival hyperaemia. Unoprostone had no clinically notable effects on vital signs, laboratory profiles, or comprehensive ophthalmic examinations. One of 659 Unoprostone 0.15%-treated patients had a change in iris colour after 12 months of monotherapy. Except for a higher incidence of burning/stinging and burning/stinging upon instillation, Unoprostone was comparable to timolol 0.5% twice daily and betaxolol 0.5% twice daily. No safety concerns were raised with use of Unoprostone as adjunctive therapy. Unoprostone had no significant effect on exercise-induced heart rate in healthy subjects or on pulmonary function in patients with mild-to-moderate asthma. The safety profile of Unoprostone 0.15% was consistent with published information on the 0.12% formulation. In conclusion, Unoprostone has an excellent safety profile in patients with POAG or OH.
Unoprostone activation of BK (KCa1.1) channel splice variants
Biochim Biophys Acta 2015 Nov;1848(11 Pt A):2859-67.PMID:26277265DOI:10.1016/j.bbamem.2015.08.005.
This investigation was conducted to study the relationship between intracellular Ca(2+) and activation of large conductance Ca(2+)-activated K(+) (BK) currents by Unoprostone, the first synthetic docosanoid. We used HEK293 cells stably transfected with two BK channel splice variants, one sensitive to Unoprostone and the other insensitive. We examined the effects of Unoprostone on channel activity in excised inside-out patches and cell-attached patches. The half-maximal stimulation of the sensitive BK channels by Ca(2+) was shifted from 3.4±0.017 nM to 0.81±.0058 nM in the presence of 10 nM Unoprostone. There was no effect on insensitive channels even at Unoprostone concentrations as high as 1000 nM. There was no effect of Unoprostone on the voltage dependence of the BK channels. Changes in open probability and effects of Ca(2+) and Unoprostone were best described by a synergistic binding model. These data would suggest that Ca(2+) and Unoprostone were binding to sites close to one another on the channel protein and that Unoprostone binding causes the affinity of the calcium binding site to increase. This idea is consistent with three dimensional models of the Ca(2+) binding site and a putative Unoprostone binding domain. Our results have important implications for the clinical use of Unoprostone to activate BK channels. Channel activation will be limited if intracellular Ca(2+) is not elevated.
A preliminary risk-benefit assessment of latanoprost and Unoprostone in open-angle glaucoma and ocular hypertension
Drug Saf 1999 Jun;20(6):505-14.PMID:10392667DOI:10.2165/00002018-199920060-00004.
Latanoprost and Unoprostone (isopropyl Unoprostone) represent the first commercially available prostaglandin analogues to be used for the treatment of glaucoma. Both compounds reduce intraocular pressure by enhancing uveoscleral outflow. Latanoprost, when used once daily in the evening, produces a greater reduction in pressure than timolol. Latanoprost produces mild conjunctival hyperaemia compared with timolol in some patients. Darkening of the irides has been reported, especially in green-brown, yellow-brown and blue/grey-brown irides. Hypertrichosis and hyperpigmentation of the eyelashes have also been demonstrated. Although latanoprost has not been proven to cause uveitis or cystoid macular oedema, case reports of an association exist. Latanoprost does not produce systemic adverse effects nor does it alter routine blood analyses. Unoprostone, when given twice daily, produces less of a reduction in intraocular pressure than timolol or latanoprost. Three times daily use may be required to approach the effectiveness of timolol. Unoprostone may have a similar adverse effect profile to latanoprost, but may to cause more corneal epithelial problems. Unoprostone is also not known to cause systemic adverse effects. Both agents are welcome additions to the treatment of glaucoma. However, additional studies and more experience are needed with each agents.