Vicatertide
Based on 1 Customer Validation
Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a Ka of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases.
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- Purity: 99.24%
- CAS No.: 1251838-01-3
- 화학식: C42H66N10O10
- 분자량:871.03
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보관:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Smad1 |
Vicatertide (SB-01) potently and selectively inhibits purified human factor XIa via a mixed allosteric mechanism, with a potency of 130 nM and an efficacy of approximately 90%. It also binds to purified human factor XI with an affinity of approximately 80 nM and forms a 4:1 hFXI::SB-01 co-complex[1].
Vicatertide acts via a mixed allosteric inhibition mechanism, which dose-dependently decreases the maximum reaction rate (Vmax) of hFXIa and slightly increases the Michaelis constant (KM)[1].
Vicatertide (Peniel 2000, P2K) (75-125 μM; coincubation with 2 ng/mL TGF-β1) selectively suppresses phosphorylation of Smad1/5/8 while moderately reducing Smad2 phosphorylation in primary bovine intervertebral disc cells, and 125 μM achieves nearly complete inhibition of p-Smad1/5/8[1].
Vicatertide (125 μM; coincubation with 2 ng/mL TGF-β1) upregulates mRNA levels of COL2A1 and ACAN in primary bovine intervertebral disc cells[1].
Vicatertide (125 μM; combined with ALK5/ALK1 selective inhibitors) elevates COL2A1 and ACAN transcription mainly via modulating ALK1-Smad1/5/8 cascade rather than ALK5-Smad2 pathway in primary bovine intervertebral disc cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary bovine intervertebral disc cells
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Concentration:125 μM
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Incubation Time:1 h preincubation with TGF-β1 plus subsequent 30 min cell incubation
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Result:Significantly increased mRNA levels of COL2A1 and ACAN after co-treatment with TGF-β1.
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Cell Line:Primary bovine intervertebral disc cells
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Concentration:25, 75, 100, 125 μM (P2K), TGF-β1 2 ng/mL
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Incubation Time:P2K preincubated with TGF-β1 for 1 h, followed by 30 min cell incubation
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Result:Selectively inhibited TGF-β1-induced Smad1/5/8 phosphorylation and mildly reduced Smad2 phosphorylation; 125 μM nearly completely suppressed Smad1/5/8 phosphorylation.
Failed to suppress TGF-β1-evoked Smad2 phosphorylation.
Vicatertide (3, 6 mg/kg; intravenous injection; single administration) significantly reduces thrombus formation in a rat model of tissue thrombin-induced vena cava thrombosis[1].
Vicatertide significantly reduces thrombus weight and thrombus incidence in mouse lung cancer models[1].
Vicatertide (Peniel 2000, P2K) (10 μg per disc; intradiscal single injection; single administration) increases %DHI values, improves MRI degeneration grade, lowers histological degeneration score, and elevates nucleus pulposus proteoglycan and collagen contents at 4/8/12 weeks after dosing in rabbit intervertebral disc degeneration models[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1251838-01-3
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Appearance Solid
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분자량 871.03
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화학식 C42H66N10O10
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Color White to off-white
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Synonyms
SB-01; Peniel 2000
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Sequence
Leu-Gln-Val-Val-Tyr-Leu-His
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Sequence Shortening
LQVVYLH
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
H2O : 6.25 mg/mL (7.18 mM; ultrasonic and adjust pH to 3 with CH3COOH)
0.02 M HCl : 2.5 mg/mL (2.87 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (279 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 (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| 0.02 M HCl / H2O | 1 mM | 1.1481 mL | 5.7403 mL | 11.4807 mL | 28.7017 mL |
| H2O | 5 mM | 0.2296 mL | 1.1481 mL | 2.2961 mL | 5.7403 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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