ISTH0036
Based on 1 Customer Validation
ISTH0036 is a phosphorothioated LNA-modified antisense oligonucleotide gapmer that potently and selectively inhibits TGF-β2 mRNA and protein expression, with IC50 values of 0.4 μM and 0.7 μM, respectively. ISTH0036 reduces choroidal neovascularization and vascular leakage, inhibits fibrosis, blocks epithelial-mesenchymal transition, suppresses angiogenesis while promoting bleb survival. ISTH0036 can be used for research on various ocular diseases, such as glaucoma and neovascular retinal diseases.
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- Purity : 96.85%
- CAS No.: 2179222-27-4
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
제품 설명
IC50 & Target
[1]|
TGF-β2 0.4 μM (IC50, mRNA) |
TGF-β2 0.7 μM (IC50, protein) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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.
- Fibrosis/Collagen Morphometry
- RNA extraction experimental
- Western Blot
- Collagen: Sirius Red Staining
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Endothelial Tube Formation Assay
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Protocol For Protein Expression And Purification
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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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
순도&문서
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Data Sheet (281 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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Handling Instructions (2242 KB)
References
[1]. Pfeiffer N, 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. Published 2017 Nov 30. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)