17-phenyl trinor Prostaglandin F2α isopropyl ester (Synonyms:比马前列素异丙酯;比马前列腺素异丙酯)
目录号 : KCM10964 CAS No. : 130209-76-6 纯度 : ≥98%
17-phenyl trinor PGF N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost. The N-ethyl amide prostaglandin prodrugs are converted to the active free acid more slowly than the analogous prostaglandin ester prodrugs such as latanoprost. This product is the isopropyl ester of the free acid prostaglandin which corresponds to Bimatoprost. The free acid, 17-phenyl trinor PGF, is a potent FP receptor agonist. In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. The 17-phenyl trinor PGF isopropyl ester derivative was examined for IOP-lowering activity during the development of latanoprost. At the dose of 3 μg/eye in the monkey, 17-phenyl trinor PGF isopropyl ester was the most potent analog tested in reducing IOP, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost. However, this derivative was also significantly more irritating to the eye than latanoprost.
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1mg
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5mg
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10mg
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10 mM * 1 mL in DMSO
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生物活性

17-Phenyl trinor PGF2α isopropyl ester is a FP receptor agonist and intraocular pressure-lowering agent. 17-Phenyl trinor PGF2α isopropyl ester induces iris sphincter contraction, reduces intraocular pressure and pupil diameter, causes no ocular irritation, and only leads to mild conjunctival hyperemia. 17-Phenyl trinor PGF2α isopropyl ester is applicable to relevant research on glaucoma.

体内研究

17 Phenyl trinor PGF2 α isopropyl ester (3 μg; single ocular local administration) can induce a statistically significant maximum 2.9 mmHg IOP reduction in cynomolgus monkeys with normal blood pressure [1].
17-Phenyl trinor PGF2 α isopropyl ester (3 μg; ocular surface administration; A single dose can cause mild eye irritation in domestic female cats.
17-Phenyl trinor PGF2α isopropyl ester (0.03-3 μg; Single ocular administration can induce dose-dependent mild conjunctival congestion in New Zealand albino white rabbits [1].

 

Animal Model: Cynomolgus monkeys
Dosage: 3 μg
Administration: o.a.; single dose
Result: Produced a maximum reduction in IOP of 2.9 mmHg.
Animal Model: Domestic female cats (2-3 kg)
Dosage: 3 μg
Administration: o.a.; single dose
Result: Caused a maximum irritation score of 0.2 arbitrary units, which was significantly lower than the irritation induced by PGF2α isopropyl ester (1b).
Animal Model: New Zealand White albino rabbits (2-3 kg)
Dosage: 0.03 μg, 0.1 μg, 0.3 μg, 1 μg, 3 μg
Administration: o.a.; single dose
Result: Induced mild conjunctival hyperemia, with maximum difference scores (experimental eye vs. control eye) of approximately 0.8, 1.0, 1.4, 1.5, and 1.7 arbitrary units at doses of 0.03 μg, 0.1 μg, 0.3 μg, 1 μg, and 3 μg, respectively; this hyperemia was significantly less pronounced than that induced by PGF2α isopropyl ester (1b).
 
分子式
C26H38O5
分子量
430.6
CAS号
130209-76-6
中文名称
比马前列素异丙酯
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (232.24 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.3224 mL 11.6122 mL 23.2245 mL
5 mM 0.4645 mL 2.3224 mL 4.6449 mL
10 mM 0.2322 mL 1.1612 mL 2.3224 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;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, 6 months; -20°C, 1 month。-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。

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