| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| 1g | |||
| Other Sizes |
Purity: ≥98%
| ln Vivo |
Anecorstat acetate, when administered intraocularly (5 μl 10% solution), markedly reduces pathological retinal angiogenesis and raises levels of PAI-1 mRNA [2].
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| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) albino rat (intravitreal injection of premixed antibiotics to affect retinal blood vessel growth) [2]
Doses: 5 μl 10% anectaline acetate suspension Route of Administration: Injection into the eye Experimental Results: Significant inhibition of the Pathological retinal angiogenesis in the model without Dramatically affecting normal intraretinal blood vessels. PAI-1 mRNA increased 6- to 9-fold 1 to 3 days after injection. To test the effect of Anecortave Acetate on retinal neovascularization, newborn Sprague-Dawley rats were placed in a variable oxygen environment (alternating 50% and 10% every 24 hours) for 14 days to induce ROP. At 14 days of age (immediately after removal from the oxygen chamber), rats received a single intravitreal injection in the left eye. Half received 5 μl of a 10% suspension of Anecortave Acetate, and the other half received 5 μl of vehicle (70:20:10 by volume, polyethylene glycol: phosphate-buffered saline: EtOH). This injection protocol was repeated in the right eye of each animal at 16 days of age. All rats were subsequently kept in room air and were euthanized at 18 days of age for retinal analysis. [1] * To determine the effect of Anecortave Acetate on normal retinal vascular development, 7-day-old rats raised in room air received an intravitreal injection of 5 μl of a 10% suspension of the drug in the left eye and 5 μl of vehicle in the right eye. Control rats received no injection. These rats were euthanized at 10 days of age for retinal analysis. [1] * For the RNase protection assay mechanism study, 14-day-old rats from the variable oxygen environment were given an intravitreal injection of Anecortave Acetate, vehicle, or nothing. They were then euthanized 1, 2, or 3 days later, and their retinas were dissected for mRNA analysis. [1] |
| References | |
| Additional Infomation |
Anecortave acetate is an organic molecular entity. Anecortave acetate (Retaane) is an analogue of corticosteroid acetate; its steroid modifications include the removal of the 11β-hydroxyl group (OH) and the addition of a 21-acetic acid ester group. Due to these modifications, Anecortave acetate lacks the typical anti-inflammatory and immunosuppressive properties of glucocorticoids. Alcon is developing and marketing Retaane. See also: Anecortave (note moved to).
Drug Indications It has been studied for the treatment of glaucoma and macular degeneration. Mechanism of Action Anecortave acetate acts as an anti-angiogenic agent, inhibiting angiogenesis by reducing the expression of extracellular proteases and inhibiting endothelial cell migration. Its anti-angiogenic activity does not appear to be mediated through any known common pharmacological receptors. (Ophthalmology 2004;111:2316-7) RETAANE blocks the signaling of multiple growth factors because it acts downstream, independently of initiating angiogenesis stimulation, and inhibits angiogenesis after angiogenesis stimulation. |
| Exact Mass |
386.209
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|---|---|
| CAS # |
7753-60-8
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| Related CAS # |
7753-60-8
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| PubChem CID |
111332
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| Appearance |
White to off-white solid powder
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| Density |
1.23g/cm3
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| Boiling Point |
551.8ºC at 760 mmHg
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| Flash Point |
188.4ºC
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| Index of Refraction |
1.572
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| LogP |
3.301
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
808
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(OCC([C@@]1([C@]2(CC=C3[C@]4(C)C(=CC(CC4)=O)CC[C@H]3[C@@H]2CC1)C)O)=O)=O
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| InChi Key |
YUWPMEXLKGOSBF-GACAOOTBSA-N
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| InChi Code |
InChI=1S/C23H30O5/c1-14(24)28-13-20(26)23(27)11-8-19-17-5-4-15-12-16(25)6-9-21(15,2)18(17)7-10-22(19,23)3/h7,12,17,19,27H,4-6,8-11,13H2,1-3H3/t17-,19+,21+,22+,23+/m1/s1 SMILES
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| Chemical Name |
17,21-Dihydroxypregna-4,9(11)-diene-3,20-dione 21-acetate
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| Synonyms |
Anecortave Acetate Anecortave Al 3789 NSC 15475 NSC 24345 Retaane Hydrocortisone Acetate EP Impurity E
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00299507 | COMPLETED | Drug: Anecortave Acetate Sterile Suspension, 30 mg/mL Drug: Anecortave Acetate Sterile Suspension, 60 mg/mL Other: Anecortave Acetate Vehicle |
Macular Degeneration | Alcon Research | 2005-03 | Phase 3 |
| NCT00489840 | COMPLETED | Drug: Anecortave Acetate Sterile suspension 15 mg Drug: Anecortave Acetate |
Chronic Central Serous Chorioretinopathy | Manhattan Eye, Ear & Throat Hospital | 2007-05 | Phase 1 Phase 2 |
| NCT00333216 | TERMINATED | Drug: Anecortave Acetate Sterile Suspension, 30 mg/mL Drug: Anecortave Acetate Sterile Suspension, 60 mg/ML Other: Anecortave Acetate Vehicle |
AMD | Alcon Research | 2005-05 | Phase 3 |
| NCT00570479 | COMPLETED | Drug: anecortave acetate | Glaucoma Uveitis, Posterior |
Texas Retina Associates | 2006-09 | Phase 1 |
| NCT00332657 | TERMINATED | Drug: Anecortave Acetate Sterile Suspension, 30 mg/mL Drug: Anecortave Acetate Sterile Suspension, 60 mg/mL Other: Anecortave Acetate Vehicle |
AMD | Alcon Research | 2006-09 | Phase 3 |
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