ISTH0036
Based on 1 Customer Validation
ISTH0036 is a phosphorothioate LNA-modified antisense oligonucleotide gapmer that selectively targets and downregulates TGF-β2 mRNA. ISTH0036 suppresses TGF-β2 expression, reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-to-mesenchymal transition, and inhibits angiogenesis while promoting bleb survival. ISTH0036 exhibits long-lasting, dose-dependent ocular tissue distribution and target engagement in rabbit and non-human primate eyes. ISTH0036 can be used for the study of various ocular disorders, such as glaucoma and neovascular retinal diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 96.85%
- CAS 番号: 2179222-27-4
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
ISTH0036 potently and specifically suppresses TGF-β2 mRNA (IC50 = 0.4 μM) and protein (IC50 = 0.7 μM) in human A172, human Panc1, human trabecular meshwork cells, and murine astrocytes[1].
ISTH0036 potently downregulates TGF-β2 mRNA in a dose-dependent manner in relevant ocular cell-based assays[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ISTH0036 (intravitreal; single dose) preserves bleb size and survival in a mouse glaucoma filtration surgery model[1].
ISTH0036 exhibits potent anti-fibrotic and antiangiogenic activity in a mouse choroidal neovascularization model[1].
ISTH0036 (intravitreal; single dose, repeated doses) induces pronounced, long-lasting dose- and time-dependent target engagement in rabbit and non-human primate ocular tissues, with target engagement lasting up to 4 months in non-human primates after a single intravitreal dose[2].
ISTH0036 exhibits potent activity in murine choroidal neovascularization models by reducing neovascularization, vascular leakage, fibrotic development, and blocking epithelial-to-mesenchymal transition[2].
ISTH0036 (intracameral; day 0, day 14; until day 28) significantly increases bleb area and prolongs bleb survival in a murine glaucoma filtration surgery model[3].
ISTH0036 (intravitreal; single dose post laser procedure) significantly reduces angiogenesis with no effect on early inflammation in a murine laser-induced choroidal neovascularization model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2179222-27-4
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性状 Solid
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Color White to off-white
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SMILES
[ISTH0036]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2242 KB)
参考文献
[1]. Pfeiffer N, Voykov B, Renieri G, et al. First-in-human phase I study of ISTH0036, an antisense oligonucleotide selectively targeting transforming growth factor beta 2 (TGF-β2), in subjects with open-angle glaucoma undergoing glaucoma filtration surgery. PLoS One. 2017;12(11):e0188899. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ISTH0036 関連分類
HY-158821 関連分類
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