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.
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- Pureté: 96.85%
- CAS No.: 2179222-27-4
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
Chemical Information
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CAS No. 2179222-27-4
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Appearance Solid
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Color White to off-white
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SMILES
[ISTH0036]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2242 KB)
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ISTH0036 Related Classifications
HY-158821 Related Classifications
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