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.
For research use only. We do not sell to patients.
- Purity: 96.85%
- CAS No.: 2179222-27-4
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Storage:
-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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2242 KB)
References
[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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